Alpha-iminobenzyl penicillins - by direct reaction of aldehydes with unisolated derivs of alpha aminobenzylpenicillin

摘要

Process for prepg. penicillins of formula:- (where (6-APA) is the 6-amino-penicillanic acid residue; R1, R2, R3 = H, halogen, NO2, dialkylamino, alkylamino, acyloxy acylamino (all. 1-6 C), alkyl (1-8 C), sulphonyl, thioalkyl, alkylsulphonyl (1-12 C), alkoxycarbonyl (1-6C), cycloalkyl (5-7 C); R4, R5 = H, alkyl, cycloalkyl, aryl, aralkyl, opt. substd. by one or more halogens) by reacting a penicillin of formula:- with an aldehyde of formula : R5.CHO in a medium at pH 4-7.5 at -30 to +45 degrees C, pref. -5 to +10 degrees C, R6 = alkyl, aryl, cycloalkyl, alkoxy. High yields of penicillins from intermediates II which need not be isolated. Products are active against Gram+ and Gram- organisms resistant to other penicillins.