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Volume 25, Issue 1
Displaying 1-34 of 34 articles from this issue
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BUDHIMAN UPADHYAY, SATISHCHANDRA TRIPATHI1977 Volume 25 Issue 1 Pages 1-5
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIon-exchange resins have been employed to separate Cr (III) and Cr (VI) present in the water decomposition product of ethereal blue perchromate prepared with 5-Sulphosalicylic acid. The quantitative estimations of Cr (III) and Cr (VI) present in cationic and anionic portions of the decomposition product have been determined by the usual Volumetric and Gravimetric methods. The experimental results and ratios between Cr (III) and Cr (VI) are in agreement with formula (CrIIISu)3[CrIII(CrVI2O7)3] for the water decomposition product corresponding to parent blue perchromate, (CrIIISu)3[CrIII(CrVI2O103], where Su is bivalent Sulphosalicylate ion.View full abstractDownload PDF (623K) -
HIROSHI HIKINO, CHOHACHI KONNO, TOSHIMI NAGASHIMA, TOMOAKI KOHAMA, TSU ...1977 Volume 25 Issue 1 Pages 6-18
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMicrobial transformation of germacrone (5) using Cunninghamella blakesleeana has resulted in the stereoselective attack of oxidation enzymes to give three optically active epoxides (6, 7, and 8) whose stereostructures have been elucidated by chemical and physicochemical evidence. Transannular cyclization of germacrone 1, 10-epoxide (6) and germacrone 4, 5-epoxide (7) by acids has been performed and it has been found that the former gives the eudesmanes (10 and 11) while the latter affords the guaianes (9 and 12-15). The mechanism of acid-induced transannular rearrangement of germacra-1 (10), 4-dienes and their epoxides is discussed.View full abstractDownload PDF (1596K) -
SHIKIFUMI KITAZAWA, HAJIME ITO, HITOSHI SEZAKI1977 Volume 25 Issue 1 Pages 19-28
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSegmental difference in the transmucosal fluid movement and its effect on the drug absorption was studied with sulfanilamide, sulfisoxazole and metoclopramide. The segments investigated were stomach, duodenum, jejunum, ileum and colon, and the ligation method was employed in the experiment of the stomach, and the reat of the segments were investigated by the simultaneous four in situ recirculation perfusions method which was devised originally in our laboratories. The results revealed that the absorption of the drugs in the stomach was not affected by the transmucosal fluid movement, while large volume of fluid secretion was observed. However, the drug absorption in the rest of the segments was affected in some extent by the fluid movement. Segmental differences in the absorption of these three drugs were also elucidated. Concerning the glucose effect, it was revealed that the effect was localized only in the upper part of the small intestine.View full abstractDownload PDF (1222K) -
CHUNGCHYI TSENG, SHIRO TERASHIMA, SHUNICHI YAMADA1977 Volume 25 Issue 1 Pages 29-40
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAiming to prepare optically active pyrrolidines (2) which are usable as chiral additives for asymmetric syntheses via enamines, and whose absolute configurations can correspond to that of D-proline (D-3c), an exploitation of the novel synthetic scheme for 2 from L-α-amino acids (L-3) via optically active γ-amino acids (4) was studied. Reaction of (S) (-)-ditosylate ((S) (-)-10a) easily derivable from L-phenylalanine (L-3a), with diethyl potassiomalonate (3.0 eq.) in tetrahydrofuran, could directly give a mixture of (R)-pyrrolidine-2-one ((R)-12a) and (R) (-)-malonate ((R) (-)-13a) in 70-80% yield. Some mechanistic studies revealed that the malonate reaction proceeded through the regiospecific ring opening of (S) (+)-aziridine ((S) (+)-11a). Acidic hydrolysis of a crude mixture of (R)-12a and (R) (-)-13a afforded (R) (-)-4a without racemization in 49% yield based on (S) (-)-10a. The same synthetic route was applicable to L-valine (L-3b), giving (R) (+)-4b. However, (S)-4c could be obtained from L-proline (L-3c), by the treatment of (S) (-)-iodide ((S) (-)-16c) prepared from (S) (-)-ditosylate ((S) (-)-10c), with malonate anion, followed by acidic hydrolysis. (R) (-)-4a and (R) (+)-4b thus obtained were readily converted into (R) (-)-2a and (R) (+)-2b by dehydration and reduction. When the asymmetric synthesis of 4-methyl-4-phenyl-2-cyclohexenone (18) was examined by using (R) (-)-2a and (R) (+)-2b, (S) (-)-18, being antipodal to that provided by using L-proline-derived pyrrolidines (1) as chiral additives, was successfully obtained.View full abstractDownload PDF (1583K) -
MUTSUYOSHI KITAMOTO, SHIRO TERASHIMA, SHUNICHI YAMADA1977 Volume 25 Issue 1 Pages 41-46
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs methods for preparing 4-acetoxy-cyclopentane-1, 3-dione derivatives (1), two synthetic schemes were examined. While the successive catalytic reduction and acetylation of cyclopentane-1, 3, 4-triones (2) according to the reported procedure gave the desired 1, the acid-catalyzed condensation of O-acetyl malic anhydride (3) with isopropenyl acetate (4a) and diethyl ketone enol acetate (4b) gave 2-carboxymethyl-5-methyl-3-oxo-2, 3-dihydrofuran (6a) and its 4-methyl derivative (6b), respectively, as the sole isolable product. The structures of 6a and 6b were elucidated from their chemical and spectroscopic behavior. Plausible formation mechanism for the compounds was also proposed.View full abstractDownload PDF (834K) -
MASAYASU YAMAMOTO, JUNKO SUGIMURA, TOYOZO UNO1977 Volume 25 Issue 1 Pages 47-49
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSQuinonedichlorodiimide (I) reacts with chinoform (5-chloro-7-iodo-8-hydroxyquinoline (II)) as well as with 7-iodo-8-hydroxyquinoline-5-sulfonic acid (III) to yield a colored compound. The chemical structure of this compound is investigated from the spectral (infrared, ultraviolet, nuclear magnetic resonance, Mass) data and the elemental analysis. The fact that both the reactions of I+II and I+III give the same compound suggests that I replaces chlorine atom and sulfonic acid group at 5-positions of II and III, respectively. The spectral data supports that the reaction product is 5-qunionediimino-7-iodo-8-hydroxyquinoline.View full abstractDownload PDF (432K) -
KAZUYA KOHASHI, TOYOSHIGE KABEYA, YOSUKE OHKURA1977 Volume 25 Issue 1 Pages 50-56
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSColor reactions of 1, 3, 5-trinitrobenzene and acetophenone in methanol and methanol-water mixtures under the Janovsky conditions were investigated by use of the stopped flow rapid scan spectrophotometric technics. The observations that the color changes in methanol were quite different from those in methanol-water mixtures of high water content were discussed in comparison with the absorption spectral features of the coloring matters (I-Na and II-Na). The color reaction pathways presented in these media were summarized.View full abstractDownload PDF (791K) -
YOSUKE OHKURA, KAZUYA KOHASHI, HIROSHI HAMADA1977 Volume 25 Issue 1 Pages 57-63
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new photometric method is presented for the assay of serum glutamate dehydrogenase activity on the basis of the determination of 2-oxoglutaric acid produced in the enzyme reaction by means of the previously established method for selective determination of the acid with diazotized sulfanilic acid. The method gives reliable results and is suitable to assay a large number of samples at the same time with 0.1 ml of sample.View full abstractDownload PDF (833K) -
SEIICHIRO YOSHIDA, TAKESHI SAKAI1977 Volume 25 Issue 1 Pages 64-68
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1. Total acetylcholine (ACh) levels in the rat whole brain homogenate decreased during the maximal tonic extension induced by bufalin. 2. "Free" ACh levels in the rat whole brain homogenate increased during the maximal tonic extension induced by bufalin, but not by pentylenetetrazol. 3. ACh release from rat cerebral cortical slices increased in a medium containing bufalin. 4. After intracerebral Hemicholinium-3 or scopolamine, 50% convulsive dose of bufalin in mice was increased, but was decreased after eserine. 5. A relationship between the convulsant effect of bufalin and its ACh-releasing effect was discussed.View full abstractDownload PDF (657K) -
MIKIHIKO KONDA, TOKURO OHISHI, SHUNICHI YAMADA1977 Volume 25 Issue 1 Pages 69-74
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFollowing the previous asymmetric syntheses of (S)-(+)-laudanosine (V) and (S)-(+)-reticuline (VI) from L-3-(3, 4-dihydroxyphenyl) alanine (L-DOPA), (R)-(-)-laudanosine (XXIV) has been also synthesized from L-DOPA. A key step is an epimerization of (1S, 3S)-methyl 1-(3, 4-dimethoxybenzyl)-6, 7-dimethoxy-1, 2, 3, 4-tetrahydroisoquinoline-3-carboxylate (XIa), which was derived from a major product of the Pictet-Spengler reaction of the methyl ester of L-DOPA (Ia) and sodium 3-(3, 4-dimethoxyphenyl) glycidate (IIa), to (1R, 3S)-isomer (XIIa) under the hydrogenation condition using PtO2 in MeOH-AcOH (100 : 1). XIa and XIIa are interconvertible under this condition. Isomerization reactions of XIa and XIIa in a basic medium (MeONa in MeOH) have been also examined. Both compounds epimerize at C-3 position and afford the new (1S, 3R)-(XIII)-and (1S, 3R)-(XIV)-isomers, respectively.View full abstractDownload PDF (815K) -
MASANORI YOSHIOKA, YUTAKA KIRINO, ZENZO TAMURA, TAKAO KWAN1977 Volume 25 Issue 1 Pages 75-78
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA detection method of radicals during photolysis of catecholamines and 3, 4-dihydroxyphenyl-L-alanine was established. Electron spin resonance spectra of the radicals derived from catecholamines under the photolytic condition showed hyperfine structures which were assigned to o-semiquinone anion radicals.View full abstractDownload PDF (542K) -
SEITARO SAEKI, AYAKO YAMASHITA, YASUHIRO MORINAKA, MASATOMO HAMANA1977 Volume 25 Issue 1 Pages 79-86
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1, 1-Ethylenedioxy-9-(2-pyridyl) quinolizidine (1) was converted to N-ethoxycarbonylpyridinium salt (3) via monohydrobromide (2) by successive treatment with ammonium bromide and ethyl bromoacetate. The reaction of 3 with hydrochloric acid was markedly affected with the concentration of the acid. Thus, when 3 was heated with 15-20% hydrochloric acid, ring closure took place accompanied by hydrolysis of the ketal and ester groups and also decarboxylation to give 17-hydroxy compound (4). Heating with triethylamine gave dehydrated pyridinium salt (5) which was reduced with sodium borohydride and then catalytically to dl-allomatridine (6). On the other hand, heating 3 with 5-10% hydrochloric acid gave a carboxylic acid (9) which was also transformed into 6 through an ester (10) and a ring closure product (11) as shown in Chart 2. The action of 30% acid on 3 followed by the similar treatments afforded 1-hydroxy-9-(2-pyridyl) quinolizidine (7). Transformation of 1 to 17-hydroxyallomatridine (8) was further achieved successively by hydrolysis to 1-oxo compound (12), formation of its cyanohydrin (13) and hydrogenation over Raney nickel.View full abstractDownload PDF (930K) -
TARO OGISO, KAZUNORI KUHARA, TAKASHI KOBAYASHI, HIROYUKI MASUDA, YOSHI ...1977 Volume 25 Issue 1 Pages 87-95
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo clarify a correlation between the fatty acid composition and the drug-metabolizing enzyme activity in liver microsomes and the action of drug for liver disease, phosphorylcholine (PC), the fatty acid composition of microsomal lipids and aminopyrine N-demethylase activity were measured during PC administration to carbon tetrachloride (CCl4)-poisoned rats. A dose of CCl4 for 2 days produced a clear per cent decrease in stearic and arachidonic acids and an increase of palmitic and oleic acids of microsomal phospholipids. The phosphatidylcholine in the poisoned rats consisted of less arachidonic and stearic acids and more linoleic acid. Administration of PC resulted in the restoration of the fatty acid content to the control levels at relatively early stage. It was found that there was a good correlation between the arachidonic acid content of the phospholipids, especially phosphatidylcholine, and the aminopyrine N-demethylase activity. Electron transfer between endogenous P-450 and NADPH added significantly dropped and the percentage of P-450 reduced with NADPH added was much smaller in CCl4-poisoned rats. These results suggest that the fatty acid composition of the phospholipids may regulate the structure of the endoplasmic membrane and phospholipids of specific structure may play an essential and functional role in oxidative demethylation in the particles.View full abstractDownload PDF (1065K) -
YOSHINOBU NAKAI, EIHEI FUKUOKA, SHINICHIRO NAKAJIMA, JIRO HASEGAWA1977 Volume 25 Issue 1 Pages 96-101
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMicrocrystalline cellulose (M.C.C.) having various ratios of crystal region to amorphous one obtained by grinding. Crystallinity was determined for M.C.C. and ground M.C.C. by X ray diffraction method (powder method) using Hermans'theory. Crystallinity was also determined by infrared measurement in converting hydroxyl groups into deuteroxyl groups in amorphous region of M.C.C. Crystallinities by both methods showed linear relationship for the samples. Specific surface area was measured by adsorption methods of nitrogen gas and water vapor for M.C.C. and ground samples. The same value of 1 m2/g was given by nitrogen gas adsorption for M.C.C. and ground samples. In water vapor adsorption ground samples increased in surface area with grinding time from 150 m2/g of intact M.C.C. to 360 m2/g of 32 hr ground M.C.C. This is due to the conversion of crystal into amorphous state by mechanical force. The linear relationships between specific surface area by water vapor adsorption and heat of wetting in water was obtained for ground samples. Porosity in compression and hardness of tablet was measured for ground samples. It was found that intact M.C.C. showed larger porosity in compression and higher tablet hardness than ground M.C.C.View full abstractDownload PDF (709K) -
KEI TSUZURAHARA1977 Volume 25 Issue 1 Pages 102-108
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe immunosuppressive and tumor-inhibitory activities in mice of cycloheximide cinnamates depended on the structure and position of a substituent on the benzene ring of the cinnamate moiety. When the levels of antibody production and tumor growth rate in the treated mice were analyzed statistically in relation to Hansch's hydrophobic constant π for each substituent, the π-response curves for the two biological responses were found to be similar to each other, suggesting that the two pharmacological activities depend on a common process which is influenced by the hydrophobicity of the cycloheximide cinnamates.View full abstractDownload PDF (723K) -
KEI TSUZURAHARA, KAZUO OGIWARA1977 Volume 25 Issue 1 Pages 109-114
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffects of cycloheximide-p-chlorocinnamate on humoral and cellular immune response in mice were investigated. The compound i) suppressed primary and secondary hemagglutinin response, ii) inhibited preferentially the production of IgG type antibodies, iii) reduced the number of hemolytic plaque forming cells in the spleen to nearly zero, and iv) suppressed the induction of delayed-type skin hypersensitivity and foot pad reaction.View full abstractDownload PDF (700K) -
SHIKIFUMI KITAZAWA, IKUO JOHNO1977 Volume 25 Issue 1 Pages 115-121
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt had been clarified in our previous study that the transmucosal fluid inflow and the absorption of sulfanilamide in alloxan diabetic rats were increased significantly than in control rats using the in situ recirculating perfusion method. The present study was designed to elucidate further in full the effects of diabetes on these intestinal absorptions. Plasma osmolality was increased with increasing blood glucose and a good correlation was obtained over a wide range of the blood glucose. The increase of blood glucose resulted in the increment of the transmucosal fluid inflow and the absorption of the drug. To examine these effects of blood glucose, rats having hyperglycemia, one of physiological characteristics in diabetic animals, were prepared by the administration of D-glucose. The fluid movement and the drug absorption in the glucose administered rats were significantly increased than in the controls and were not found significant difference compared to those of the diabetics on the basis of dry-weight of the small intestine of the experimental animal. From the results obtained in the present study and in our previous findings, it might be able to conclude that a possible mechanism on the increase of the drug absorption in the diabetics would be that the enhancement of plasma osmolality due to the hyperglycemia caused the increment of the transmucosal fluid inflow to compensate the abnormal high osmolality in blood and this inflow might lead the drug absorption increase consequently.View full abstractDownload PDF (980K) -
KENJI OZAWA, TAKAYUKI SHIOIRI, SHUNICHI YAMADA1977 Volume 25 Issue 1 Pages 122-125
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe diphenyl phosphorazidate (DPPA) method, a new coupling procedure in the peptide synthesis, was successfully applied to the synthesis of Z-His(Z)-Ser-Asp(OBut)-Gly-Thr-Phe-OBut (I) corresponding to sequence 1-6 of secretin. Comparison of the DPPA method with the classical azide method was made by the fragment coupling of Ser-Asp with Gly-Thr-Phe, revealing that the former may be as good as the latter.View full abstractDownload PDF (597K) -
SHIKIFUMI KITAZAWA, TETSUO KOMURO1977 Volume 25 Issue 1 Pages 126-134
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe present work was designed to make clear the effect of plasma volume expanders on both the transmucosal fluid movement, that is, fluid absorption through the epithelial layer of the small intestine, and the intestinal sulfanilamide absorption in fasted rats, with particular attentions to homeostatic fluid transfer within body. Arterial hematocrit value of the subjected animal was measured during the course of the intestinal perfusion experiments and employed to monitor intensively the homeostatic fluid transfer. The circulation volume expansion induced by an infusion of a fresh plasma obtained from non-fasted healthy donnor rats produced a rise in both the fluid and sulfanilamide absorption from intestine, whereas infusions of commercial expanders showed an opposite result, that is, the transmucosal fluid absorption decreased with a reduction in the drug absorption from intestine. Although a transfusion solution is said to serve for an improvement of the body fluid environment up to the normal in a dehydrated situation as a fasting, any plasma volume expander may not have always a definite effect on the intestinal absorption in fasted rats. From these results, it was suggested that body fluid enviroment, or physiological conditions concerning extracellular body fluids should be taken into considerations in studying the gastrointestinal absorption in rats. And some discussions were made to evaluate the plasma volume expanders.View full abstractDownload PDF (1123K) -
KUSUO NARITA, MINORU SEKIYA1977 Volume 25 Issue 1 Pages 135-140
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to shed light on the previous confused data reported for the constant-boiling liquids for the formic acid-trialkylamine system, vapor-liquid equilibria for a representative formic acid-triethylamine system under a number of pressures were examined by the use of a modified still designed for this purpose. The diagrams obtained and the pressure dependence of the azeotropic compositions clearly indicate azeotropic features. Precise composition of the maximum azeotrope was determined for this system as well as for other formic acid-trialkylamine systems.View full abstractDownload PDF (758K) -
SHIKIFUMI KITAZAWA, TETSUO KOMURO1977 Volume 25 Issue 1 Pages 141-146
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffect of fasting and prosperity or decay of serum proteins of rats were studied with electrophoretic and other techniques. Total concentration of serum protein decreased progressively during fasting, and at the same time volume of the circulating serum was also observed to decrease. These results reflected in a rise in arterial hematocrit value. As for compositions of blood serum, about 45% of albumin was lost during three-day-fasting, whereas an amount of globulins lost during the same periods of fasting was about 37%. Among globulins, α2-, β- and γ-fractions were observed to decrease significantly. These decays might bring about some alterations in a mode of drug transfer in the body. Using these serums in vitro equilibrium dialysis was performed. Serum protein binding of sulfamethoxazole had a tendency to decrease with increasing periods of fasting, probably due to a fall in the concentration of serum albumin in fasted rats. Reduction in the amount of proteins of blood serum, particularly albumin, was assumed to affect the drug transfer in body and some discussions about the drug efficacy in fasted rats were made.View full abstractDownload PDF (848K) -
AKIRA KONO, YOSHIKAZU MATSUSHIMA1977 Volume 25 Issue 1 Pages 147-150
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAspartate aminotransferase from a water soluble fraction of pig heart muscle was irradiated with 60Co γ-ray, 274 and 380 nm light in aqueous solutions with or without radioprotective amines, i.e. 2-mercaptoethylamine (MEA) and 2-aminoethylisothiuronium bromide (AET). For γ-irradiation, the enzyme was quite sensitive (D37, 37.5 krad) and was effectively protected by the amines against the radiation-inactivation. The change in protein structure judged from gel electrophoretic pattern was also improved by MEA. The 380-nm irradiation caused inactivation, which was least protected by MEA, without serious changes in the protein structure. Photochemical degradation of pyridoxal phosphate was supposed to be responsible for the inactivation. MEA protects apoenzyme probably as a radical scavenger.View full abstractDownload PDF (534K) -
KAZUSHIGE MORIMOTO, TSUTOMU YAMAHA, MASAHIRO NAKADATE, IKUO SUZUKI1977 Volume 25 Issue 1 Pages 151-157
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (771K) -
SHIGENORI HARADA, MINORU SAWADA, MASAHIKO CHIKUMA, AKIRA YOKOYAMA, HIS ...1977 Volume 25 Issue 1 Pages 158-162
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThioacetoacetanilide (I) was prepared through β, β-dimercaptobutyranilide by addition of H2S to acetoacetanilide. The acid dissociation constants (pKa) of I and thiothenoyltrifluoroacetone (II) were determined spectrophotometrically to be 6.21±0.03 and 4.38±0.09 in 50% acetonitrile, respectively. The pseudo-first order rate constant for the hydrolyses of I and II were (1.55±0.28)×10-2 and (2.92±0.11)×10-4 min-1 in 50% acetonitrile, respectively. They depended on the concentration of water, but not on pH over 1-7 and 1-5, respectively. The related compounds, thiobenzoylacetanilide, thiodibenzoylmethane and benzoylthioacetone were also investigated similarly for comparison. The former was hydrolyzed but the latter two were oxidized to form the disulfides. The introduction of phenyl group instead of methyl group into the β-position seems to make the β-thiol group resistant against the hydrolysis or the oxidation.View full abstractDownload PDF (618K) -
SHIU KIYOSAWA, TOSHIO KAWASAKI1977 Volume 25 Issue 1 Pages 163-165
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree kinds of pregnane derivatives G5, G6, and G7 were isolated from the aerial parts of Dioscorea tenuipes FRANCH. et SAVAT. They were characterized as 2β, 3α, 4β-trihydroxy-5β-pregn-16-en-20-one (IV) and its 2-(VII) and 4-monoacetates (VIII), respectively, which are corresponding to coexisting diotigenin (I) and its monoacetates (II and III).View full abstractDownload PDF (487K) -
CHUNGCHYI TSENG, SHIRO TERASHIMA, SHUNICHI YAMADA1977 Volume 25 Issue 1 Pages 166-170
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the course of our examinations on an applicability of the novel synthetic scheme for optically active pyrrolidines from L-α-amino acids, it was found that the reaction of (R) (-)-2-phenyl-1-tosylaziridine ((R) (-)-9) with diethyl potassiomalonate exclusively afforded (S) (+)-pyrrolidine-3-carboxylate ((S) (+)-10) as a mixture of two diastereoisomers by the attack of malonate anion at the C2-carbon of the aziridine ring. This result is completely different from those obtained for (S)-2-benzyl or isopropyl-1-tosylaziridine ((S)-7a, b) on which the attack of malonate anion occurred specifically at the unsubstituted C3-carbon. These results clearly show that electronic effect of the C2-substituent is considered as the most important factor which controls regiospecificity of the ring opening of 2-substituted-1-tosylaziridines by malonate anion. Structual confirmation of (S) (+)-10 was also carried out by converting it into (S) (+)-3-phenylpyrrolidine ((S) (+)-17).View full abstractDownload PDF (699K) -
ISOO ITO, TAISEI UEDA, YOSHIO KUROYANAGI, KENJI SUZUKI1977 Volume 25 Issue 1 Pages 171-174
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSyntheses of some pyridoxine derivatives having a thiazoline ring or a thiazolium ring at the 5-position are described. 3-(3-Hydroxy-4-hydroxymethyl-2-methyl-5-pyridyl)-methyl-5-methylthiazoline-2-thione (IX) was synthesized from α4, 3-O-isopropylideneisopyridoxamine (VII), carbon disulfide, ammonium hydroxide, and chloropropanone. Similarly X, XI, and XII were obtained by employing appropriate alkyl chloride instead of chloropropanone. Treatment of IX, X, XI, and XII with 30% hydrogen peroxide and 35% hydrochloric acid gave 3-(3-hydroxy-4-hydroxymethyl-2-methyl-5-pyridyl) methyl-4-methyl-5-substitutedthiazoliumchloride hydrochlorides (XIII, XIV, XV, XVI).View full abstractDownload PDF (530K) -
MASAYOSHI HORIOKA, TOSHINOBU AOYAMA, HIRONOBU KARASAWA1977 Volume 25 Issue 1 Pages 175-178
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe pharmacological effect of propantheline bromide (PB) mixed with dried aluminum hydroxide gel (DAHG) was investigated in guinea-pigs and human. In guinea-pigs, antimuscarinic effect was tested in their isolated ileums, and in human, salivary secretion was measured by Herxheimer. It was found that coadministration of PB together with DAHG resulted in a loss of potency of PB due to degradation, and thus the effects of powdered preparations of PB mixed with DAHG were merely those of antacids alone. But antimuscarinic agents kept away from antacids showed no change in their efficacy.View full abstractDownload PDF (545K) -
YOSHIO KANEDA, AKIRA YAMAJI, MASAHIRO IWAIDA, YOSUKE OHKURA1977 Volume 25 Issue 1 Pages 179-181
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCaptan and difolatan, widely used fungicides, decomposed rapidly when irradiated with light of a low pressure mercurry lamp to cis-4-cyclohexene-1, 2-dicarboximide.View full abstractDownload PDF (469K) -
MITSURU FURUKAWA, TADASHI OKAWARA, YURIKO TERAWAKI1977 Volume 25 Issue 1 Pages 181-184
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOptically active N-benzylidene-R(+)- and S(-)-α-methylbenzylamines (1b, c) were allowed to react with dichlorocarbene to give optically active α-methylbenzylamine-α-chloro-α-phenylacetamides (3b, c), and the ratio of diastereomers was R-R : S-R=73 : 27 and S-S : R-S=79 : 21, respectively.View full abstractDownload PDF (526K) -
TAKAKO WATANABE, KAZUYA KAMIJO1977 Volume 25 Issue 1 Pages 185-191
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe activity of histaminase by using histamine as a substrate was spectrophotometrically estimated as the hydrazone derivative of imidazole acetaldehyde with 2, 4-dinitrophenylhydrazine (DNP). The measurement of enzyme activity in pig kidney was based on oxygen consumption in the presence of histamine by means of oxygen electrode, and the assay based on hydrazone derivative was performed with a spectrophotometer. In determination of oxygen consumption, there was a remarkable difference in the patterns of activities under the conditions of incubation temperature of 38°and 60°. The maximum activity of histaminase at 60°was about 2.4 times higher than that at 38°when the concentration of histamine was 10-4M. By measuring the absorbance of the hydrazone derivative of imidazole acetaldehyde formed in the presence of 3×10-4M histamine at 60°, it could be compared with oxygen consumption proportional to an increased amount of enzyme. Isooctane extractable hydrazones and unreacted DNP disturbed markedly the spectrophotometric assay, but these substances could be removed by use of a mixed solvent of isooctane and CHCl3. If aldehyde compound is formed over 1 μM/min or if oxygen is consumed over 15μM/min even in the incubation temperature of 38°, it is indicated that hydrazone derivative of aldehyde compound can be spectrophotometrically detected and that the assay method can be applied to the measurement of histaminase activity.View full abstractDownload PDF (871K) -
HIROSHI HASEGAWA, HEIHACHIRO ARAI, HIROSHI IGETA1977 Volume 25 Issue 1 Pages 192-195
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of N-acetyliminopyridazinium ylide (3) with benzyne afforded 1, 3-dipolarcycloadduct (4). Photolysis of the cycloadduct (4), having alkoxy group in the 3-position of the pyridazine ring, afforded α-alkoxynaphthalene (5), and 3-(2-acetoamidophenyl) pyridazine (7). Photolysis of 4a did not give naphthalene, but afforded indazolo [2, 3-b] pyridazine (6). Reaction of 4 with base afforded 3-vinylindazole (8). indazolo [2, 3-b]4, 5-dihydropyridazine (9). Reaction of 2H-pyridazinone 1-oxide (22) with benzyne afforded the 1, 3-cycloadduct (23), followed by fission of N-O bond to give pyridazinone substituted with 2-hydroxyphenyl group (24). The reaction mechanisms are also discussed.View full abstractDownload PDF (477K) -
TOSHIKAZU NOZOYE, TATSUYA NAKAI, AKINORI KUBO1977 Volume 25 Issue 1 Pages 196-198
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of 2-indolinone (I) with acetaldehyde was carried out in the presence of dimethylaniline and afforded the epimeric mixture of 2-oxoindolin-3-ethylidenes in good yield. The epimeric 2-oxoindolin-3-ethylidenes were successfully separated to give pale yellow needles (II), mp 173-174°(15%) and bright yellow needles (III), mp 147-148.5°(38%). The configurations of II and III were assigned Z and E respectively on the basis of their 1H- and 13C-NMR spectral data.View full abstractDownload PDF (490K) -
HIROMU SAKURAI, SHIGERU SHIMOMURA, KAZUHIKO ISHIZU1977 Volume 25 Issue 1 Pages 199-201
Published: January 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe model system, which showed previously the hydroxylations to aniline and p-toluidine, consisting of hemin, cysteine and pyridine exhibited very similar absorption and EPR spectra to cytochrome P-450 at 293 and 77°K. From the spectral properties the axial cysteinate S-Fe-N (pyridine) coordination is necessary to show a low-spin state of porphyrin at 293°K. In the presence of trace amount of pyridine, a transition of the high-spin state observed at 293°K to the low-spin state of porphyrin was detected at 77°K.View full abstractDownload PDF (437K)
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