YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
チオクト酸およびその関連化合物の合成研究 (第9報)
チオクト酸誘導体とビタミンB1との結合化合物の合成 その1
出口 義雄中西 和夫
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ジャーナル フリー

1963 年 83 巻 7 号 p. 701-704

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Both thioetic acid and thiamine play important rôle in the metabolic process of pyruvic acid and preparation of their conjugate would be significant for biological studies. The present series of synthetic work was undertaken in order to obtain such compounds.
Attempt was first made to synthesize a compound in which the sulfur atoms in 6- and 8-positions of thioctlc acid was bonded in disulfide-form to thiamine. Application of sodium thiosulfate to methyl 6, 8-dichloroöctanoate (VI) to obtain the Bunte salt (VII) showed that chlorine in 6-position is less reactive and, by the use of the methyl ester (VIII) and amide (XIV) of 6-bromo-8-chloroöctanoic acid, the objective 6, 8-bis{2-{N-[(4-amino-2-methyl-5 -pyrimidinyl) methyl] formamido}-1-(2-hydroxyethyl) propenyldithio}-octanoic acid was obtained as its methyl ester (II) and amide (IV). Although II retained its thioctic acid activity in approximately 90% of the original acid, transition of thiamine into blood cells was hardly observed.

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© by the PHARMACEUTICAL SOCIETY OF JAPAN
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