申请人:Rhone-Poulenc Sante
公开号:US04593101A1
公开(公告)日:1986-06-03
1,2,3,4-Tetrahydro-4-quinolinone of formula: ##STR1## are prepared from a 3-anilinopropionic acid of formula: ##STR2## which is treated successively with phosgene, phosgene in the presence of dimethylformamide, a Lewis acid or a strong acid, and a base. In the formula (I) and (II), R denotes a hydrogen atom, a halogen atom or an alkyl (1 to 4 carbon atoms) or alkoxy (1 to 4 carbon atoms) radical, and R.sub.1 denotes a hydrogen atom or an alkyl radical (1 to 4 carbon atoms). The compounds of formula I are useful as intermediates in the production of known drugs.
公式为##STR1##的1,2,3,4-四氢-4-喹啉酮可以从公式为##STR2##的3-苯胺基丙酸经过苯酰氯、苯酰氯与二甲基甲酰胺、路易斯酸或强酸、以及碱的连续处理制备而成。在公式(I)和(II)中,R表示氢原子、卤素原子或烷基(1到4个碳原子)或烷氧基(1到4个碳原子)基团,R.sub.1表示氢原子或烷基基团(1到4个碳原子)。公式I的化合物在已知药物的生产中作为中间体是有用的。