发明名称 A-AULKYL (OR ARYL) THIO-5-HYDROXYTRYPTOPHAN DERIVATIVE AND THE PREPARATION PROCESS THEREOF
摘要 <p>1440468 Tryptophan derivatives SAGAMI CHEMICAL RESEARCH CENTER 28 Feb 1974 [1 March 1973] 9155/74 Heading C2C Novel compounds (I) are made by reacting (III) with compounds of formula in acid conditions (where R is alkyl or aryl, Z and Y are protective groups, X is -CHO or and each R<SP>1</SP> is alkyl or taken together signify alkylene). (I) can be converted to 5-hydroxy-tryptophan (IV), e.g. #-(5-benzyloxyindolyl-3)-α-acetylamino -α- methylthiopropionic acid methanethiol ester is heated under reflux in ethanol containing NEt 3 to give methyl #-(5-benzyloxyindolyl - 3) -α- acetylamino -α- methylthiopropionate which is debenzylated using Raney Ni to give methyl #-(5-hydroxy-indolyl-3)-α- acetylaminopropionate (V), the acetate of which is prepared; (V) is heated under reflux in 10% H 2 SO 4 to give (IV). 5,5-Dimethyl-2-amino-1- methyl - sulphinyl - 1 - methylthio - 1 - pentene (obtained by interacting formaldehyde dimethyl mercaptal S-oxide and 4,4-dimethoxybutyronitrile) is treated with acetic anhydrideacetic acid to give 5,5-dimethoxy-2-acetylamino- 2-methylthiovaleric acid methanethiol ester.</p>
申请公布号 CA1018985(A) 申请公布日期 1977.10.11
申请号 CA19740193799 申请日期 1974.02.28
申请人 SAGAMI CHEMICAL RESEARCH CENTER 发明人 TSUCHIHASHI, GENICHI;OGURA, KATSUYUKI
分类号 C07D209/20 主分类号 C07D209/20
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