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TSUGIO SHIMAMOTO, YOSHIHARU TSUBOTA
1968 Volume 16 Issue 6 Pages
965-971
Published: June 25, 1968
Released on J-STAGE: March 31, 2008
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Even if a random distribution of particles has been achieved in the practical process, a precise quantity of an active ingredient in individual dose units can not be always assured. This variation in the potency is attributed to a problem of mixing and related directly to the sampling error. Theoretical consideration indicates that the variance in the proportion of an active ingredient developed through sampling from a randomized bulk mixture is calculated with the following equations ; 1. When the shape of particles is spherical [numerical formula] 2. When the shape of particles is cubic [numerical formula] where, P is the proportion of an active ingredient, g the sample weight, d
A and d
B are the the densities of components, L
A and L
B the mean volume diameters of components, σ
A and σ
B the standard deviations of particle-sizes distributions of components ; suffix A means the active component. The possible application of the result to suspension and emulsion has been discussed.
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MITSUJI YANAI, TOSHIO KINOSHITA, SHIGEKO TAKEDA
1968 Volume 16 Issue 6 Pages
972-976
Published: June 25, 1968
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A structual study of so-called dihydrocompound and tetrahydrocompound of 10H-pyridazino (3, 2-b) quinazolin-10-one (VI) was described. These two compounds were assigned to be 3, 4-dihydro- and 1, 2, 3, 4-tetrahydro-10H pyridazino (3, 2-b) quinazolin-10-one (III, IV), respectively. Catalytic hydrogenaytion of VI and III revealed that while the former gave II, III, IV and IX, the later gave II and IX.
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OSAMU NAGASE, HIROAKI TAGAWA, MASAO SHIMIZU
1968 Volume 16 Issue 6 Pages
977-983
Published: June 25, 1968
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Four pantethine analogs (homopantethine (VII), α-methyl-(XIIIb) and β-methyl-pantethine (XIIIc), and oxypantetheine (XVI)) were prepared. Synthesis of VII from D-pantothenonitrile (I) and homocysteamine by using the thiazine derivative (III) as an intermediate was established. XIIIb and XIIIc were synthesized by the thiazoline method described previously, and XVI by the general method.
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YASUSHI ABIKO, KINYA KAMEDA, MASAO SHIMIZU
1968 Volume 16 Issue 6 Pages
984-987
Published: June 25, 1968
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α-Methylpantethine, β-methylpantethine, homopantethine and oxypantetheine did not support the growth of L. bulgaricus B1 which required pantethine for its growth. These pantethine analogs were competitive inhibitors of pantethine in this microorganism, but they stimulated the bacterial growth at their subinhibitory concentrations in the presence of a small amount of pantethine. Magnitudes of their inhibitory effects were in the order of oxypantetheine≥homopantethine>β-methylpantethine>α-methylpantethine on the molar basis of the reduced form.
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KOTARO TAKAHASHI, SHUICHI MIYASHITA
1968 Volume 16 Issue 6 Pages
988-996
Published: June 25, 1968
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1) Two new ozonolysis products of anhydromethyldihydrousnic acid monoacetate were proved to have structures Va and VI. 2) The mechanism of the formation of the three ozonolysis products, II, Va and VI from anhydromethyldihydrousnic acid monoacetate was discussed.
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HIROYOSHI YAMAGUCHI
1968 Volume 16 Issue 6 Pages
997-1002
Published: June 25, 1968
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Wenn N, N-Dimethylthiopropionamid-S-phenacylbromid mit Salicylaldehyd in Acetanhydrid umgesetzt wird, so entsteht ein unbekannter roter Farbstoff. Bei der Ermittlung zeigte es sich, daβ es sich um [Benzo-3-methyl-α-pyranyl-(2)]-[5-phenyl-1, 3-oxathiolium]-methyl-methin-bromid handelt.
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TETSUJI KAMETANI, TOYOHIKO KIKUCHI, KEIICHIRO FUKUMOTO
1968 Volume 16 Issue 6 Pages
1003-1008
Published: June 25, 1968
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1-(4-Hydroxy-3-methoxybenzyl)-6, 7-dimethoxy-2-methyl-1, 2, 3, 4-tetrahydroisoquinolin-8-ol (V) was oxidized with potassium ferricyanide to dienone (VI), which was subjected to dienone-phenol rearrangement with hydrochloric acid in acetic acid to give the cularine type compound (XXI). These reactions provide a possible model for biogenesis of cularine and related alkaloids. Moreover, this paper described the preparation of V.
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YOSHIRO KOBAYASHI, CHIGEN AKASHI
1968 Volume 16 Issue 6 Pages
1009-1013
Published: June 25, 1968
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The reactions of difluorotriphenylphosphorane with alcohols were studied, and the former substance was found to be an excellent one-step flourinating reagent for substituting the hydroxyl group of primary and secondary alcohols. When more than one mole equivalent of alcohols were added to the reagent, the corresponding ethers were also obtained.
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YASUO INUBUSHI, YOSHISUKE TSUDA, TAKESHI KONITA, SAICHI MATSUMOTO
1968 Volume 16 Issue 6 Pages
1014-1018
Published: June 25, 1968
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An alkaloid constituent of "Chukanso"( ?? ?? ?? ), a kind of the Chinese drug "Shih-Hu"( ?? ?? ) was examined and a new alkaloid which was designated as shihunine was isolated. From degradative and spectroscopic data, it was established that the structure of shihunine should be represented by the Formula (F).
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HIROYUKI INOUYE, TOSHIO ARAI
1968 Volume 16 Issue 6 Pages
1019-1022
Published: June 25, 1968
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Das Aglucon des Tetrahydromonotropein-methylesters ergab bei der Saurebehandlung nicht ein Anhydrid, sondern eine Furan-Verbindung (VIII), wodurch die R-Konfiguration des asymmetrischen Zentrums 8 im (VII) und somit im Monotropein bewiesen wurde.
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YUKIO KAMEDA, TAIJYU KURAMOTO, KATSUHIKO MATSUI, TAKAKO EBARA
1968 Volume 16 Issue 6 Pages
1023-1029
Published: June 25, 1968
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In order to study the enzymatic properties of α-amino acylase of KT 801 (Pseudomonas sp.), which has δ-ornithine acylase, purification of the α-amino acylase have been attempted. α-Amino acylase of KT 801 was extracted by means of spheroplast formation and purified by fractionation with ammonium sulfate, acrinol treatment, and CM Sephadex chromatography. The specific activity of the purified enzyme toward N-benzoyl-L-alanine was 2500 μM/hr/mg and it was represented about 70 fold purification over the original cell suspension. This enzyme has a pH optimum around 8.0 toward benzoyl-L-alanine. It has an optical specificity and hydrolyzes benzoyl-L-amino acids. Also, it hydrolyzes α-N-benzoyl-L-amino acids but not phenylacetyl amino acids. The ratio of the activities toward α-N-benzoyl amino acids remained constant all through the purification steps except for 2-N-benzoyl-L-ornithine. These results suggest that one enzyme hydrolyze these α-N-benzoyl amino acids. Then, the α-amino acylase of KT 801 was provisionally named "benzoylamino acid amidohydrolase."
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MITSUYOSHI MATSUO
1968 Volume 16 Issue 6 Pages
1030-1033
Published: June 25, 1968
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The syntheses of DL-allylglycine (2-
14C,
15N), DL-homomethionine (2-
14C,
15N), DL-homomethionine (G-
3H), 3-methylthiopropionamide (1-
14C) and 4-methylthiobutyramide (1-
14C) were described.
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MITSUYOSHI MATSUO, MIKIO YAMAZAKI
1968 Volume 16 Issue 6 Pages
1034-1039
Published: June 25, 1968
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Some labelled compounds were fed to horseradish leaves (Armoracia lapathifolia GILIB.) and yellow mustard seeds (Brassica juncea COSSON). DL-Homomethionine (2-
14C,
15N) was directly incorporated into sinigrin in comparison with the other labelled compounds, however DL-allylglycine (2-
14C,
15N) was incorporated insignificantly and DL-methionine (2-
14C), sodium acetate (2-
14C) and sodium malonate (2-
14C) were incorporated without randomization. The relationships of their efficient precursors were discussed on sinigrin biosynthesis. Chemical degradation of the allyl thiourea derived labelled mustard oil was described.
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HIROMICHI SAEKI, TADAHIRO IWASHIGE, EIJI OHKI
1968 Volume 16 Issue 6 Pages
1040-1047
Published: June 25, 1968
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Solvolysis of 2, 3-di-O-benzyl-5-O-mesyl-6-O-trityl-D-glucofuranose (IV) was carried out under an oxide ring migration, affording methyl 2, 3-di-O-benzyl-α-L-altrofuranoside (XVIIIa) and its β-anomer (XVIIIb) in a ratio of 1 : 2.2.
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KIYOSHI SAKAI, SADAO OIDA, EIJI OHKI
1968 Volume 16 Issue 6 Pages
1048-1055
Published: June 25, 1968
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Base-catalyzed cyclizations of glutaraldehyde with nitroethane, β-nitropropionic acid, β-nitro-α-methoxypropionic acid, and methyl vinyl ketone were investigated. The structures of these resulting nitrocycloalkanols were determined by NMR analysis and chemical reactions.
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JUNKO MORITA, DAISUKE SATOH
1968 Volume 16 Issue 6 Pages
1056-1061
Published: June 25, 1968
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Hydrolysis of pentaacetylgitoxin (I) with diastase gave selectively 3', 3'', 3''', 16-tetraacetylgitoxin (IIa) as a main product. When IIa was treated with potassium hydrogen carbonate, acetyl groups were successively eliminated in the order of those at C-3''', -16, -3'' or -3' positions to afford 3', 3'', 16-triacetylgitoxin (IIc), 3', 3''-diacetylgitoxin (IId), 3'-monoacetylgitoxin (acetylgitoxin-γ, IIe) and gitoxin (IIf). These partial acetates did not agree with those obtained in acetylation of gitoxin (IIf), in which acetyl groups were introduced in the order at C-4''', -16, -3''' or -3' positions. The partial acetates obtained by the former method (deacetylation) were thought to be more essential for the study of metabolism of I than those prepared by the latter method (acetylation).
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SADATAKE KATO, KUNIO KURATA, TAKAO WAKABAYASHI, YOSHIHIKO SUGISAWA
1968 Volume 16 Issue 6 Pages
1062-1064
Published: June 25, 1968
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Radioactive sodium 5-acetamido-2, 4, 6-triiodo-N-methyl-isophthalamate (
131I) was synthesized by isotopic exchange reaction in acidic aqueous solution. When this compound was injected intravenously into rabbit, it was excreted very rapidly and little of it was taken up by organs except kidney. The blood clearance of the compound obtained by external counting after the single injection was exponential after a certain period of equilibrium and its rate was independent of the administered dose. Those results indicate that this substance is filtered at the glomeruli passively and the half clearance time can be considered to be a parameter of the renal glomerular filtration rate.
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EIGO TAKABATAKE, TOSHIHIKO ARIYOSHI, KATSUHIRO SCHIMIZU
1968 Volume 16 Issue 6 Pages
1065-1069
Published: June 25, 1968
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Effect of the pretreatment with tolbutamide in female rats on the liver microsomal activation (anticholinesterase activities) and degradation (formation of p-nitrophenol) of parathion was studied. Both pathways were stimulated by tolbutamide-pretreatment, but the degradation process was superior to the activation of parathion at lower concentration of substrate in the liver preparation of rats pretreated with tolbutamide. The formation of p-nitrophenol from paraoxon by liver homogenate was also accerelated by tolbutamide. These facts should be reflected in the lowering of parathion toxicity in animals pretreated with tolbutamide.
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TOSHIO KAWASAKI, TATSUO YAMAUCHI
1968 Volume 16 Issue 6 Pages
1070-1075
Published: June 25, 1968
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Prosapogenins, B and A, which are provided together with prosapogenin-C (diosgenin β-D-glucopyranoside) (II) on partial hydrolysis of dioscin (diosgenin 2-O- and 4-O-bis-α-L-rhamnopyranosyl-β-D-glucopyranoside=diosgenin β-chacotrioside) (I) were characterized as 4-O-(III) and 2-O-α-L-rhamnopyranosyl-β-D-glucopyranoside (IV), respectively. A glycoside found along with dioscin, gracillin and other spirostanol glycosides in the rhizoma of Dioscorea Tokoro MAKINO was isolated and identified with prosapogenin-B of dioscin on the basis of paper, thin-layer and, for the first time, gas liquid chromatographic comparisons and chemical evidence. The difference of the site of the probable enzymatic cleavage in the sugar portion (chacotriose) of dioscin from that of the splitting by acid hydrolysis was noted.
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YOSHIYASU FURUKAWA, MIKIO HONJO
1968 Volume 16 Issue 6 Pages
1076-1080
Published: June 25, 1968
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9-β-D-Ribofuranosyladenine was synthesized by condensation of N
6-octanoyladenine (I) with 1-O-acetyl-2, 3, 5-tri-O-benzoyl-β-D-ribofuranose (II) or 1, 2, 3, 5-tetra-O-acetyl-β-D-ribofuranose (III) in sym-dichloroethane or chlorobenzene in the presence of Friedel-Crafts catalysts followed by hydrolysis of the acyl groups. By this procedure the formation of the corresponding anomer was not observed Similarly, 9-β-D-ribopyranosyladenine was synthesized from I and 1, 2, 3, 4-tetra-O-acetyl-β-D-ribopyranose, and 9-β-D-ribofuranosylguanine in high yield from N
2-palmitoylguanine and III.
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HIROSHI HIKINO, SHUJI TAKAHASHI, YOJIRO SAKURAI, TSUNEMATSU TAKEMOTO, ...
1968 Volume 16 Issue 6 Pages
1081-1087
Published: June 25, 1968
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From zedoary, Curcuma zedoaria (Zingiberaceae), has been isolated a new sesquiterpenic keto-dioxide, zederone. Chemical and physicochemical studies of it and its derivatives permit the allocation of the structure I to it.
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HIROSHI HIKINO, KEITARO AOTA, YASUO TOKUOKA, TSUNEMATSU TAKEMOTO
1968 Volume 16 Issue 6 Pages
1088-1090
Published: June 25, 1968
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Cyperotundone (I), a constituent of nutgrass (Cyperus rotundus (Cyperaceae)), has been converted by exposure to Corlicium sasakii into its oxygenated congeners, sugeonol (II), another constituent of nutgrass, and isopatchoul-4-en-3-on-8α-ol (III : R=H)) whose stereostructure has been deduced by its spectral properties.
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SATOSHI KAWAI, ZENZO TAMURA
1968 Volume 16 Issue 6 Pages
1091-1094
Published: June 25, 1968
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Gas chromatographic assay of the catecholamines in urines and tumor was successfully carried out using the procedure described in the previous paper. Gas chromatographic method was superior to fluorometry as regards selectivity. Each catecholamine was analysed simultaneously and the whole pattern of chromatogram permitted a rapid, simple diagnostic evaluation. Moreover the resolving power of gas chromatography led to a finding of a co-existing unknown substance, which had the identical retention time to dopa and existed in a significant amount in normal urine, as well as in the urine of a patient with pheochromocytoma.
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TETSUJI KAMETANI, KAZUMI OHKUBO, SEIICHI TAKANO
1968 Volume 16 Issue 6 Pages
1095-1097
Published: June 25, 1968
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Phenolic oxidation of p-cresol in an electric current of 0.0025 A/cm
2 using lead as an electrode and 1 N H
2SO
4 as an electrolyte afforded three compounds, (II), (III), and (IV), which were assigned by spectral elucidation. Furthermore, an authentic sample (III) was synthesized by Ullmann reaction of p-cresol with 4-benzyloxy-3-bromotoluene, followed by hydrolysis of V with hydrobromic acid in acetic anhydride.
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ISAO SUGIMOTO
1968 Volume 16 Issue 6 Pages
1098-1104
Published: June 25, 1968
Released on J-STAGE: March 31, 2008
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Effect of 1 : 1 complex formation with a nonabsorbable drug (A) and an absorbable one (B) on the absorption of B from rat small intestine according to the recirculating perfusion method in situ was described. The combination of drugs used as the model compounds was riboflavin phosphate (A)-sulpyrin (B), riboflavin phosphate (A)-caffeine (B), riboflavin phsophate (A)-4-aminoantipyrine (B), aminopropylon (A)-sulfamethizole (B), and aminopropylon (A)-sulfisomidine (B). The absorption rate constant of B was influenced by the incorporation of A and the rate was shown to be slowed and dependent on the concentration of A. The effect was rationalized and effectively quantitated by hypothesizing that the complex AB was absorbed little or not absorbed, and that only the noncomplexed form of the absorbable drug was observably absorbed. Complexation of B with A decreased the apparent partition coefficient of B. It is thought that this suggests one possible mechanism for the absorption of complex.
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NOBUMASA IMURA, TAKASHI TSURUO, TYUNOSIN UKITA
1968 Volume 16 Issue 6 Pages
1105-1109
Published: June 25, 1968
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Uridine was benzylated with benzyl bromide in the presence of sodium hydride in dimethyl sulfoxide or dimethylformamide to give two products. The one was a dibenzyl uridine (I), yield 33%, and the other N
3-benzyluridine (II), yield 30.5%. The product (I) was converted to the product (II) by catalytic hydrogenation and was identified with N
3, 2'-O-dibenzyluridine which was synthesized by detritylation of N
3, 2'-O-dibenzyl-3', 5'-di-O-trityluridine (IV) derived by the similar benzylation of the known 3', 5'-di-O-trityluridine (III).
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KIYOMI KIKUGAWA, FUMIKO SATO, TAKASHI TSURUO, NOBUMASA IMURA, TYUNOSIN ...
1968 Volume 16 Issue 6 Pages
1110-1115
Published: June 25, 1968
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2'-O-Benzyl-4-methylthiouridine (III) and 2'-O-benzylcytidine (VI) were obtained by respective treatment of 4-methylthiouridine (II) and cytidine (V) with benzyl bromide in the presence of sodium hydride. By this reaction, highly specific benzylation of 2'-hydroxyl group of the ribonucleosides was achieved. The both compounds (III) and (VI) could easily be converted to 2'-O-benzyluridine (IV) which is an important intermediate in the synthesis of oligonucleotide.
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SHUZO TAKAGI, TOYOSHI KATAGI, KEIKO TAKEBAYASHI
1968 Volume 16 Issue 6 Pages
1116-1120
Published: June 25, 1968
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A method for the separation of alkaloids of Amaryllidaceae by a gas chromatographic technique is described. The separation of trimethylsilyl derivatives of the alkaloids was carried out using a number of commercially available non-polar and polar stationary phases, with a hydrogen flame ionization detector system. An excellent resolution of a 12 components mixture was obtained with an HI-EFF 8B column. Application of this method to the extract of the alkaloids of Lycoris radiata HERB. was also investigated.
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SHUZO TAKAGI, TOYOSHI KATAGI, KEIKO TAKEBAYASHI
1968 Volume 16 Issue 6 Pages
1121-1123
Published: June 25, 1968
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A method for the quantitative determination of lycoramine and galanthamine in the bulbs of Lycoris radiata HERB. by gas liquid chromatography using a HI-EFF 8B column was described. And the change of the amounts of these alkaliods were analyzed in every months through a year.
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SHIGENOBU OKUDA, KAORU ABE, MASAYUKI ONDA
1968 Volume 16 Issue 6 Pages
1124-1127
Published: June 25, 1968
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MITSUYOSHI MATSUO
1968 Volume 16 Issue 6 Pages
1128-1129
Published: June 25, 1968
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HIROMICHI SAEKI, TADAHIRO IWASHIGE
1968 Volume 16 Issue 6 Pages
1129-1132
Published: June 25, 1968
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TOSHIO OGINO, TAKASHI HAYASAKA, SHO ITO
1968 Volume 16 Issue 6 Pages
1132-1133
Published: June 25, 1968
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SHIGEHARU INOUYE
1968 Volume 16 Issue 6 Pages
1134-1137
Published: June 25, 1968
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TETSUJI KAMETANI, KUNIO OGASAWARA
1968 Volume 16 Issue 6 Pages
1138-1139
Published: June 25, 1968
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MASAO KONOSHIMA, HYUNGJOON CHI, KIYOSHI HATA
1968 Volume 16 Issue 6 Pages
1139-1140
Published: June 25, 1968
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KENNOSUKE SAKURAI, EIICHI YOSHII, HIDEKAZU HASHIMOTO, KIICHI KUBO
1968 Volume 16 Issue 6 Pages
1140-1143
Published: June 25, 1968
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HISAO YAMAGUCHI, TAKASHI MAEDA, TOSHIHIKO OKAMOTO
1968 Volume 16 Issue 6 Pages
1145-1148
Published: June 25, 1968
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TOSHIO NAMBARA, MITSUTERU NUMAZAWA, HIROI TAKAHASHI
1968 Volume 16 Issue 6 Pages
1148-1151
Published: June 25, 1968
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MORIO IKEHARA, MASAKATSU KANEKO, MASARU SAGAI
1968 Volume 16 Issue 6 Pages
1151-1153
Published: June 25, 1968
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TOSHIHIKO OKAMOTO, YASUYOSHI TORIGOE, MORIYUKI SATO, YO ISOGAI
1968 Volume 16 Issue 6 Pages
1154-1156
Published: June 25, 1968
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YUKIHIRO SHOYAMA, TOSHIO FUJITA, TATSUO YAMAUCHI, ITSUO NISHIOKA
1968 Volume 16 Issue 6 Pages
1157-1158
Published: June 25, 1968
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EIICHI YOSHII, MASAKI YAMASAKI
1968 Volume 16 Issue 6 Pages
1158-1159
Published: June 25, 1968
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AKIHIRO OHTA
1968 Volume 16 Issue 6 Pages
1160-1161
Published: June 25, 1968
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SHU KIYOSAWA, MASAKAZU HUTOH, TETSUYA KOMORI, TOSHIHIRO NOHARA, ICHIRO ...
1968 Volume 16 Issue 6 Pages
1162-1164
Published: June 25, 1968
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TATSUO YAMAUCHI, YUKIHIRO SHOYAMA, YOKO MATSUO, ITSUO NISHIOKA
1968 Volume 16 Issue 6 Pages
1164-1165
Published: June 25, 1968
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