Antiarrhythmic dialkyl amino alkyl benzamidines - prepd. from a benzamidine and a primary tertiary alkylene diamine

摘要

Amidines of formula (I) and their acid addition salts are newIn (I) R1R2 & R3 = H, halogen, methyl, lower alkoxy, phenoxy, benzyloxy, phenoxypropoxy, nitro, amino or CF3; R4 and R5 = lower alkyl, benzyl or together with the N atom, form a heterocycle such as pyrrolidino, piperidino or morpholino; n = 2-4). (I) are anti-arhythmic agents and loca anaesthetics and have better therapeutic ratio than procainamide. A typical compound is p-nitro-N-(2-diethylaminoethyl) benzamidine dihydrochloride. This was prepd. from 6.045g p-nitro-benzamidine hydrochloride and 3.48g 2-diethylaminoethylamine in ethanol at room temperature or at reflux. The yield was 80% mpt. 202 degrees C.