3-(Tri-substd. benzoyl) propionic acids - as relaxants or spasmolytics for the gall bladder

摘要

Cpds (I) and their salts. (where R1 is 1-4C alkyl or alkoxy or OH, R2 and R3 are such 1-4C alkyl or alkoxy OH, halogen 1-4C alkylthio, or R2+R3 is 1-3C alkylenedioxy provided that when R1 is alkoxy =1 of R2 and R3 is alkoxy or alkylthio or R2+R3 is alkylenedioxy, when R1 is alkyl or OH, R2 and R3 are alkoxy or alkylthio or R2+R3 is alkylenedioxy; when R2 and R3 are MeO, R1 is 2-3 C alkyl, 2-4C alkoxy or OH and when R2 is Me and R3 is MeO, R1 is 2-4C alkoxy) are prepd by reacting a trisubstd benzene with a reactive ester of succinic acid or its nitrile and opt. hydrolysing the product to give free COOH hydrogenating the corresponding alpa beta-unsatd acid, hydrolysing the corresponding mono- or di-ester or nitrile and cleaving a gp R1=ether to give R1=OH. Thus, 1,2,4-triethoxybenzene with succinic anhydride in the presence of AlCl3 gave (I, R1=R2=R3=EtO).