发明名称 OPTICALLY ACTIVE ALPHA-AMINOKETONE AND PRODUCTION THEREOF
摘要 NEW MATERIAL:An optically active compound expressed by formula I (mark ¦indicates asymmetric carbon; R<1> is 3-8C alkyl or phenyl; R<2> is H or lower alkyl or R<1> and R<2> together form a 5-membered ring) and an acid addition salt thereof. EXAMPLE:(S)-2-Amino-3-methyl-1-phenylbutan-1-one hydrochloride. USE:Useful as an intermediate for producing medicines and agricultural chemicals, e.g. compounds expressed by formula II (R<3> and R<4> are lower alkyl or together form 5--7-membered ring; n is 2 or 3), etc., having glutamic acid blocking action or central muscle relaxant action or as a starting raw material for optical active beta-aminoalcohols, expressed by formula III and used as an optical resolving agent. PREPARATION:An optically active amino acid expressed by formula IV as a raw material is converted into an acid addition salt of an optically active alpha-amino acid halide expressed by formula V (X is halogen), which is subjected to the Friedel-Crafts reaction with benzene in the presence of a Lewis acid, e.g. AlCl3, etc., to afford the aimed compound expressed by formula I.
申请公布号 JPS62209058(A) 申请公布日期 1987.09.14
申请号 JP19860052859 申请日期 1986.03.11
申请人 NIPPON CHEMIPHAR CO LTD 发明人 MAZAKI MITSUO;MORIFUJI NAOYA;TAKAHASHI TOSHIHIRO;HASHIMOTO KOICHI;TAKEDA HIROMITSU
分类号 C07D207/08;B01J27/00;B01J27/08;B01J27/125;C07B53/00;C07B61/00;C07C67/00;C07C213/00;C07C215/30;C07C221/00;C07C225/16 主分类号 C07D207/08
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