| 摘要 |
N-(2-(2-Oxo-azetidin-4-yl)-propionyl)-isoquinoline, benzoxazine or benzothiazine-(thi)one derivs. of formula (I) and their salts are new. Q = N-contg. benzo-heterocyclic gp. of formula (i): benzene ring B is opt., substd.; R1 = opt. protected lower hydroxyalkyl; X = O or S; Y = O, S, CH2 or opt. substd. imino; Z = opt. substd. methylene. Ring B is opt. substd. by 1-4 of halogen, lower alkyl, lower alkoxy and aryl; Y = O, S, CH2 or imino (opt. substd. by lower alkyl, acyl or aralkoxycarbonyl); Z = methylene (opt. substd. by 1 or 2 of opt. substd. 3-7C alkylene, opt. substd. 1-20C alkyl, opt. substd. 4-7C cycloalkyl, aryl, aralkyl and heterocyclyl); the 3-position of the azetidinone gp. has S-configuration; R1 = opt. protected 1-hydroxyethyl; R3 = 2-thioxopyrrolidin-4-yl. Esp. Z = pentamethylene-substd. methylene or dibutyl-substd. methylene.
|
