PROCESS FOR PREPARING PYRROLE DERIVATIVES

摘要

Pyrrole derivs. I [R1 = H, alkyl, phenyl 2-pyridyl; R2 = H, alkyl, R3,R4 = alkyl, cycloalkyl; NR3R4 = heterocycle were prepd. Thus (Me2CH)2NCH2CH2C(CO2Et)2NHAc were hydrolyzed and decarboxylated to (Me2CH)2NCH2CH2CH(NH2)CO2H, which was amidated via an Me ester and treated with (MeCOCH2)2 to give I derivs. (II). At 50 mg/kg orally in dogs, II gave 90% inhibition of ventricular arrhythmia. Also at 50 mg/kg day orally for 5 days in baboons, II inhibited blood platelet aggregation.