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Volume 18, Issue 7
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HIDEOMI FUKUDA, KAZUO WATANABE, YOSHIHISA KUDO1970 Volume 18 Issue 7 Pages 1299-1304
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA comparative study of the effect of berberine and its 9-substituted compounds (I, R=OH ; II, berberine, R=OCH3 ; III, R=OC4H9 ; IV, R=OC5H11 ; V, R=OC8H17 ; VI, R=OC12H25) on blood pressure of rats showed that substitution of OC4H9 or OC5H11 for OCH3 of berberine prolonged the transient hypotensive activity of berberine, whereas substitution by OH caused a slight hypertension. The dose of III or IV, which caused hypotension, was found to inhibit cardiac function in rats, whereas II had no effect on it. II, III, and IV decreased the beating rate in isolated perfused toad heart. Only II was found to have acetylcholine-potentiating action in frog muscle as well as guinea-pig small intestine in vitro. In the same preparations III and IV, contrariwise, inhibited acetylcholine action. In spinal rats, any response in blood pressure was not observed after the injection of each of the test compounds. From these results, possible mechanism of action of the test compounds is discussed.View full abstractDownload PDF (989K) -
CHAUYANG CHEN, HARUHIKO YAMAMOTO, TAKAO KWAN1970 Volume 18 Issue 7 Pages 1305-1309
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCatalytic hydrogenation of sodium D-xylo-5-hexulosonate (sodium 5-keto-D-gluconate) and its acid has been investigated on nickel, ruthenium, rhodium and palladium with or without boron-modification. It was found that nickel and palladium catalysts produce more L-idonate than D-gluconate especially when the metals are prepared by treating their salts with sodium borohydride. Two adsorbed models for the substrate were presented to account for the observed hydrogenation selectivity, and the role of boron at the surface was discussed in terms of complexing with two hydroxyls of L-idonate.View full abstractDownload PDF (581K) -
SADAO AOYAMA, KANZO SASAKI1970 Volume 18 Issue 7 Pages 1310-1326
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe syntheses of linearly disposed progesterone and testosterone analogues are described. On the way of the syntheses, a plausible reaction path for the catalytic hydrogenation of the α, β-unsaturated ketone (11a) to the saturated ketone (20a) is discussed. The stereochemistry of the alumina catalysed condensation products of 3β, 20β-diacetoxy-8, 9-seco-5α-pregnane-8, 9, 11-trione, not fully established in the previous paper, has been determined in the light of accumulated nulear magnetie rlsonanel (NMR) data.View full abstractDownload PDF (1853K) -
YUKIHIRO SHOYAMA, TATSUO YAMAUCHI, ITSUO NISHIOKA1970 Volume 18 Issue 7 Pages 1327-1332
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe original cannabinoids including Δ2-tetrahydrocannabinolic acid (THCA), cannabidiolic acid (CBDA), cannabichromenic acid (CBCA), and a new component, cannabigerolic acid monomethyl ether (CBGAM) were isolated with simple column chromatographic technique from the fresh Cannabis of the domestic strain. Cannabinolic acid (CBNA), observed in the stored Cannabis, was synthesized from THCA by means of ultraviolet (UV) light irradiation, and artificial conditions to yield CBNA from THCA, comparing with Δ3-isomer, were investigated.View full abstractDownload PDF (723K) -
HARUAKI YAJIMA, HIROKI KAWATANI, HIDEHIKO WATANABE1970 Volume 18 Issue 7 Pages 1333-1339
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs an example of peptide fragment condensation on the polymer support, synthesis of the tryptophan-containing decapeptide, ACTH-(5-14) was undertaken. First, suitable conditions to esterify Boc-Lys (Z)-Pro-Val-Gly-OH onto the copolymer of styrene and 2% divinylbenzene were examined. At room temperature, fairly good esterification of this tetrapeptide was achieved by the use of the bromomethylated copolymer and dicyclohexylamine. The peptide-resin was then treated with 1N HCl and triethylamine. To the resulting free tetrapeptide-resin, Z-Glu (OBzl)-His-Phe-Arg (NO2)-Trp-Gly-OH was condensed by means of DCC and the growing peptide resin was treated with HF. The product, H-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-OH was obtained simply by column chromatography on CM-cellulose.View full abstractDownload PDF (898K) -
HIROSHI IGETA, TAKASHI TSUCHIYA, CHISATO OKUDA, HIDEHARU YOKOGAWA1970 Volume 18 Issue 7 Pages 1340-1346
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN-Oxidation of 3, 3'-bipyridazines (I, X, XXV) was carried out to form the corresponding N-oxides (II, III, XI, and XII). Reaction of the bipyridazines (I, X, and XX) with POCl3-PCl5 afforded the corresponding trichloromethyl compounds (VIII, and XXV) from I and XX, and the polychloro compounds (XVIII, and XIX), in which the chlorine atoms were substituted in the rings, from X. Treatment of the bipyridazine N-oxides (II, III, and XXI) with POCl3, which have methyl groups α or γ-positions to the N-oxide groups, gave the corresponding chloromethyl compounds (VI, VII, and XXIII). And the reaction of the bipyridazine N-oxides (II and V) with Ac2O afforded the corresponding acetoxy compounds (IV and III). In conclusion, the pattern of reactions of the 3, 3'-bipyridazines and their N-oxides seems to be approximately analogous to that of monomeric pyridazines and their N-oxides.View full abstractDownload PDF (862K) -
TADAKAZU MURATA, YOSHIO IMAI, TAKEO HIRATA, MASUO MIYAMOTO1970 Volume 18 Issue 7 Pages 1347-1353
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to isolate the hypocholesterolemic principle, the neutral ethyl acetatesoluble fraction of the methanol extract of Alismatis Rhizoma was fractionated in parallel with the biological test. Thus new compounds alisol A (1), alisol B (2), alisol A monoacetate (3), alisol B monoacetate (4) and alisol C monoacetate (5) were obtained. The compounds 1, 3, 4 and 5 were shown to be effective in the test with rats.View full abstractDownload PDF (795K) -
TADAKAZU MURATA, MASUO MIYAMOTO1970 Volume 18 Issue 7 Pages 1354-1361
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSChemical studies on the structures of alisol A (1) and its monoacetate (2), the new hypocholesterolemic triterpenes of Alismatis Rhizoma, are described.View full abstractDownload PDF (997K) -
KAZUHIDE KAMIYA, TADAKAZU MURATA, MASAO NISHIKAWA1970 Volume 18 Issue 7 Pages 1362-1368
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe X-ray analysis on alisol A (23, 24)-acetonide 11-monobromoacetate was undertaken establishing the molecular structure to be 1. The usefulness of applying the least-squares method at an early stage for distinguishing real atoms from spurious peaks in the maps of minimum functions was again demonstrated.View full abstractDownload PDF (854K) -
TADAKAZU MURATA, MASAKAZU SHINOHARA, MASUO MIYAMOTO1970 Volume 18 Issue 7 Pages 1369-1384
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSStudies on the structures of alisol B, alisol B monoacetate and alisol C monoacetate, the new biological-active triterpenes of Alismatis Rhizoma, are reported. The former two compounds have been correlated to alisol A (1) establishing their structures as shown 2 and 4, respectively. The structure of alisol C monoacetate has been clarified to be 16-oxoalisol B 23-monoacetate (21) on the basis of correlation of the compound with 4. Stereochemical courses and mechanisms of some epoxide cleavage reactions of 2, 4 and alisol B diacetate (8) are also described.View full abstractDownload PDF (1742K) -
SADAO NISHIGAKI, KAZUKO OGIWARA, KEITARO SENGA, SHINOBU FUKAZAWA, FUMI ...1970 Volume 18 Issue 7 Pages 1385-1393
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe condensation of 4-substituted 6-amino-2-methylpyrimidines with diethyl ethoxymethylenemalonate, followed by thermal cyclization in Dowtherm A, yielded the corresponding 4-substituted 2-methyl-5-hydroxypyrido [2, 3-d] pyrimidine-6-carboxylates. These latter compounds served as starting materaials for several transformation reactions.View full abstractDownload PDF (939K) -
HARUAKI YAJIMA, KOICHI KAWASAKI, HIDEO MINAMI, HIROKI KAWATANI, NARIAK ...1970 Volume 18 Issue 7 Pages 1394-1401
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHuman β-melanocyte-stimulating hormone (MSH), H-Ala-Glu-Lys-Lys-Asp-Glu-Gly-Pro-Tyr-Arg-Met-Glu-His-Phe-Arg-Trp-Gly-Ser-Pro-Pro-Lys-Asp-OH (I), was synthesized by deformylation of [21-Nε-formyllysine]-human-β-MSH (IX) by hydrazine acetate. This formyl derivative (IX) was prepared by coupling reaction of Boc-Ala-Glu (OBut)-Lys (Boc)-Lys (Boc)-Asp (OBut)-Glu (OBut)-Gly-pentachlorophenyl ester and H-Pro-Tyr-Arg-Met-Glu-His-Phe-Arg-Trp-Gly-Ser-Pro-Pro-Lys (For)-Asp-OH (II) followed by treatment with trifluoroacetic acid. The latter partially protected pentadecapeptide (II) is the synthetic intermediate of monkey β-MSH (J. Am. Chem. Soc., 90, 527 (1968) ; Chem. Pharm. Bull. (Tokyo), 17, 1229 (1969)) structurally related to human β-MSH. By column chromatography on silica, the former protected heptapeptide active ester was isolated in pure form from the reaction mixture of dicyclohexylcarbodiimide-pentachlorophenol complex and Boc-Ala-Glu (OBut)-Lys (Boc)-Lys (Boc)-Asp (OBut)-Glu (OBut)-Gly-OH, which was prepared by the coupling reaction of Boc-Ala-Glu (OBut)-Lys (Boc)-Lys (Boc)-NHNH2 and H-Asp (OBut)-Glu (OBut)-Gly-OH by the azide procedure. The synthetic human β-MSH and the formyl derivative (IX) exhibited the in vitro MSH activity of 6.2×109 and 3.4×109 units/g respectively.View full abstractDownload PDF (1041K) -
AKIRA TAKAMIZAWA, HIROSHI HARADA1970 Volume 18 Issue 7 Pages 1402-1407
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of 1, 2, 4-thiadiazolium salts with dialkyl acylphosphonates (II) afforded ring expanded products, 1, 2, 4-thiadiazine derivatives. In the reaction of 4-(4-amino-2-methyl-5-pyrimidinyl) methyl-3-methyl-1, 2, 4-thiadiazolium bromide hydrobromide (VII) with dialkyl benzoylphosphonates (IIb, c), however, 10a (1-dialkylphosphoroyl) benzyl-4, 5, 10, 10a-tetrahydro-3, 8-dimethyl-1, 2, 4-thiadiazolo [4', 5'-1, 2] pyrimido [4, 5-d] pyrimidine (VIIIb, c) were obtained as major products and the 1, 2, 4-thiadiazine derivative (IX) as a minor product. Acid treatment of VIIIb, c gave XIb, c, which were intermediates of the reaction of the thiadiazolium salt (VII) with phosphonate (IIb, c), and these were converted to VIIIb, c and IX by alkaline hydrolysis.View full abstractDownload PDF (765K) -
TSUTOMU IRIKURA, YOSHINARI HASEGAWA, HAJIME KAWASAKI, TAKAAKI TOYODA, ...1970 Volume 18 Issue 7 Pages 1408-1413
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome azachalcones (3-(substituted cinnamoyl) pyridine and its 1-oxide) were synthesized. Their antitumor activity on Yoshida sarcoma and rat ascites hepatoma AH-13, AH-66 and AH-7974 was determined. 2-Chloroazachalcone, 3-chloroazachalcone, 2-chloroazachalcone 1-oxide and 3-chloroazachalcone 1-oxide were found to be curative to AH-13, AH-66 and AH-7974 but negative to Yoshida sarcoma. A few experiments to elucidate the mechanism of antitumor effect of azachalcones were performed. Effects of 3-chloroazachalcone on the growth and on the content of DNA, RNA and protein of ascites hepatoma AH-66 was observed.View full abstractDownload PDF (622K) -
SUMINORI UMIO, KAZUO KARIYONE, KUNIHIKO TANAKA, TEIJI KISHIMOTO, HITOS ...1970 Volume 18 Issue 7 Pages 1414-1425
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA number of de-chloro and de-nitro derivatives of pyrrolnitrin and the isomers as to the positions of the substituents were prepared and their antimicrobial activities were evaluated. Among the homologues having a nitro group, pyrrolnitrin has shown the strongest activity, in which the nitro group is suffered from steric hindrance. 2-Methyl-4-(2-nitro-3-chlorophenyl) pyrrole (10a) was also as effective as pyrrolnitrin. On the other hand, the de-nitro derivatives, 3-chloro-4-(3-chlorophenyl) pyrrole (8o), 3-chloro-4-(3-bromophenyl) pyrrole (8g) and 3-chloro-4-(3-trifluoromethyl) pyrrole (8t), showed stronger antimicrobial activities and broader spectra.View full abstractDownload PDF (947K) -
Conformational Changes in Fused Hydrazines, 2, 3, 5, 10-Tetrahydro-1H-pyrazolo [1, 2-b] phthalazinesAKITADA NAKAMURA1970 Volume 18 Issue 7 Pages 1426-1430
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSConformational changes of 2, 3, 5, 10-tetrahydro-1H-pyrazolo [1, 2-b] phthalazines (Va, Vb), which have a 6/5 fused ring system with two bridgehead nitrogen atoms, were studied by means of variable-temperature nuclear magnetic resonance (NMR) spectroscopy. It is concluded that they exist as the conformer VI with trans-fused configuration, converting between the two antipodes (IX, IX') via synchronous inversion of both nitrogens. The activation parameters (Ea, log A, ΔFc*) for the inversion were also determined as follows. For Va ; Ea=16.9kcal/mole, log A=16.7, ΔFc*=12.4 kcal/mole. For Vb ; Ea=18.7 kcal/mole, log A=18.3, ΔFc*=12.5 kcal/mole.View full abstractDownload PDF (524K) -
YOSHIHIRO NISHIKAWA, MAMORU TANAKA, SHOJI SHIBATA, FUMIKO FUKUOKA1970 Volume 18 Issue 7 Pages 1431-1434
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree species of lichens belonging to Umbilicaria, i.e., U. angulata, U. caroliniana, and U. polyphylla, have been examined for their water-soluble polysaccharide consitituents by chemical and physico-chemical methods. The results showed that they contained a partially O-acetylated pustulan as a sole water-soluble polysaccharide. All the polysaccharide specimens obtained here showed a remarkable antitumour effect against the implanted Sarcoma-180 in mice.View full abstractDownload PDF (580K) -
MASAYUKI ONDA, KAORU ABE, KYOKO YONEZAWA, NAOFUMI ESUMI, TERUO SUZUKI1970 Volume 18 Issue 7 Pages 1435-1439
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBocconine, one of the nematocidal alkaloids from Bocconia cordata, has been investigated by means of the nuclear magnetic resonance spectroscopy and the nuclear Overhauser effect measurements to establish the structure.View full abstractDownload PDF (512K) -
HARUHIRO FUJIMOTO, OSAMU TANAKA1970 Volume 18 Issue 7 Pages 1440-1445
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3β-Acetoxyhexakisnordammaran-20-one (V) was prepared from hydroxyhopanone (II) through IV, VI, VII, VIII, IXc and XII. Since the total synthesis of II has already been performed, the present transformation provides the total synthesis of the basic skeleton of dammarane-type triterpene.View full abstractDownload PDF (715K) -
MICHIKO MIYAKI, BUNJI SHIMIZU1970 Volume 18 Issue 7 Pages 1446-1456
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAlkyl and glycosyl migration reactions of N-1, N-3, N-7 and N-9 substituted derivatives of adenine, N6, N6-dimethyladenine, N2-acetylguanine and purine were demonstrated. In addition, the chemical shifts of these derivatives in nuclear magnetic resonance (NMR) were determined and the frontier π-electron densities of nitrogens in purine ring were calculated by simple LCAOMO method. These results provided the order of thermodynamical stability and kinetical favour of the derivatives on the alkylation reaction.View full abstractDownload PDF (1246K) -
TAKEO HIGASHINO, EISAKU HAYASHI1970 Volume 18 Issue 7 Pages 1457-1464
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSKetone carbanion reacted as nucleophilic reagent with 4-chloropyrido [2, 3-d] pyrimidine (I). Reaction of I in the presence of sodium amide with acetophenone and acetone gave 2-(4-pyrido [2, 3-d] pyrimidinyl) acetophenone (III) and 1-(4-pyrido [2, 3-d] pyrimidinyl)-2-propanone (IV), respectively. The reaction with propiophenone, 3-pentanone and 2-butanone afforded 4-ethylpyrido [2, 3-d] pyrimidine (V). The reaction with 2-pentanone gave 1-(4-pyrido [2, 3-d] pyrimidinyl)-2-pentanone (VII) and 4-propylpyrido [2, 3-d] pyrimidine (VI). Quinazoline (XIII) has been shown to add several nucleophilic reagents across the 3, 4-position. These investigation have now been extended to pyrido [2, 3-d] pyrimidine (X). The reaction of X with methylmagnesium iodide, benzylmagnesium chloride and phenylmagnesium bromide afforded 4-methyl-(XIVa), 4-benzyl-(XIVb) and 4-phenyl-3, 4-dihydropyrido [2, 3-d] pyrimidine (XIVc), respectively. These compounds was derived to 4-methyl- (IX), 4-benzyl- (XVII) and 4-phenyl-pyrido [2, 3-d] pyrimidine (XVIII), respectively, by oxidation with potassium ferricyanide in alkali medium. The reaction with acetophenone in sodium methoxide solution afforded 2-(3, 4-dihydro-4-pyrido [2, 3-d] pyrimidinyl) acetophenone (XV). The reaction with hydrogen cyanide afforded 3, 4-dihydro-4-pyrido [2, 3-d] pyrimidinecarbonitrile (XVI) which was derived to 4-pyrido [2, 3-d] pyrimidinecarbonitrile (XIX). XIX was also derived to 4-methoxypyrido [2, 3-d] pyrimidine (XX) and 4 (3H)-pyrido-[2, 3-d] pyrimidinone, respectively from the reaction with methoxide and hydroxide ion. It may be concluded through the foregoing experimental results that the addition is occured across the 3, 4-position as similar as that of XIII already reported.View full abstractDownload PDF (900K) -
TOMISHIGE MIZOGUCHI, KEISUKE SHIGEZANE, NORIO TAKAMURA1970 Volume 18 Issue 7 Pages 1465-1474
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA modified solid phase method for peptide synthesis employing haloacyl polystyrene resins is described. For this purpose, several kinds of haloacylated copolystyrene-divinylbenzene were prepared, of which the bromoacetyl derivative was of choice. Protected amino acids could be attached to or released from this type of resin more smoothly than in the case of the benzyl type. Protected amino acids and their amide, hydrazide and ester derivatives were obtained by cleavage of the amino acid resins (III) by means of alkaline aqueous dioxane, sodium thiophenoxide in dimethylformamide, methanolic ammonia, hydrazine hydrate in methanol or methanol containing a catalyst under mild reaction conditions. This modification was successfully applied to syntheses of several small peptides. Although the overall yields were slightly lower than in the original solid phase method, the peptides and their C-terminal amide derivatives could be prepared easily with preservation of all the protecting groups on them. Therefore, this method may also be useful for the preparation of peptide fragments in larger polypeptide synthesis.View full abstractDownload PDF (1301K) -
YUICHI KANAOKA, KAZUHIKO ITOH, EISUKE SATO, AKIHIKO NOMURA, YOSHIHISA ...1970 Volume 18 Issue 7 Pages 1475-1477
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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YOSHIO SASAKI, MIYOKO SUZUKI1970 Volume 18 Issue 7 Pages 1478-1482
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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TETSUJI KAMETANI, SATOSHI HIBINO, SEIICHI TAKANO1970 Volume 18 Issue 7 Pages 1482-1484
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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HIROSHI HIKINO, TAEKO TAKAHASHI, SHIGENOBU ARIHARA, TSUNEMATSU TAKEMOT ...1970 Volume 18 Issue 7 Pages 1488-1489
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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GOH MIYAJIMA, YOSHIO SASAKI, MIYOKO SUZUKI1970 Volume 18 Issue 7 Pages 1489-1491
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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TOHRU UEDA, HIROMICHI TANAKA1970 Volume 18 Issue 7 Pages 1491-1493
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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HIRONOBU ICHIKAWA, TAKENORI TANIMURA, TERUMI NAKAJIMA, ZENZO TAMURA1970 Volume 18 Issue 7 Pages 1493-1495
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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KOICHI KITANI, KAZUHIRO IMAI, ZENZO TAMURA1970 Volume 18 Issue 7 Pages 1495-1496
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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HIROSHI IGETA, TAKASHI TSUCHIYA, TOSHIKO NAKAI, GENZO OKUSA, MICHIKO K ...1970 Volume 18 Issue 7 Pages 1497-1499
Published: July 25, 1970
Released on J-STAGE: March 31, 2008
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