发明名称 1-PHENYLTHIO-2-AMINOPROPANE DERIVATIVE
摘要 NEW MATERIAL:A compound of formulaI(R<1> is halogen; R<2> is H or halogen; R<3> is methyl, ethyl or hydroxyethyl) and an acid addition salt thereof. EXAMPLE:1-(4-Cholorphenylthio)-2-propanone. USE:A preventing agent and remedy for obesity and diabetes, having inhibitory action on mammalian ingestion, enhancing action on the tolerance to saccharide, etc. with low toxicity without the exciting action on the central nervous system, safe even in use for a long term, and having improved stability with good absorption even by the oral administration. PROCESS:A compound of formula II is reacted with chloroacetone to give a compound of formula III, which is then aminated reductively to afford the compound of formulaI. The reductive amination reaction is carried out preferably by using lithium cyanoborohydride, etc. in the presence of a compound of the formula R<3>NH2 in an amount of 2-20mol based on one mole compound of formula III is a solvent, e.g. methanol, in the presence of hydrochloric acid, sulfuric acid or acetic acid.
申请公布号 JPS5788162(A) 申请公布日期 1982.06.01
申请号 JP19800164862 申请日期 1980.11.21
申请人 TAKEDA YAKUHIN KOGYO KK 发明人 MEGURO KANJI;MATSUO TAKAO
分类号 A61K31/135;A61P3/04;A61P3/08;A61P3/10;C07C67/00;C07C313/00;C07C323/25 主分类号 A61K31/135
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