Amidines preparation - by reacting silylated amides or lactams with ammonia or amines

摘要

Optionally substituted amidines are prepared by (a) silylating an amide or lactam (pref. with hexamethyldisilazane in the presence of trimethylchlorosilane or an ammonium salt) and (b) reacting the resulting silyl derivative with ammonia or a primary or secondary amine or a salt thereof in the presence of a tertiary base and of a Lewis acid as catalyst. This gives amidines which are pharmaceuticals useful as antidiabetics, antiprotozoals, antibacterials, cytostatics, local anaesthetics and virustatics. The new (and claimed) compound 2-(DELTA 2-imidazolin-2-yl)-5-nitro-thiazole has antifungal and antibacterial activity.