PROCESS FOR THE PREPARATION OF SUBSTITUTED 2-AMINOBENZIMIDAZOL

摘要

Antiviral 2-amino-1,5(6)-substd. benzimidazoles I and II [R= alkyl, cycloalkyl, Ph, furyl, thienyl; R1(in the 5- or 6-position) CO2H, (un)substd. carbomoyl, CH2OH, cyano, NO2, alkyl, alkoy, alkylthio, MeSO2, PhS, PhS(O), PhO, CF3, esterified CO2H, 1-carbalkoxy-alkyl, acyl, 1-(alkoxyimino)alkyl, 1-alkylidinealkyl, R3C(:CR4 R5) or R3C(OH)(CHR4R5) (R3=H, hydrocarbyl; R4 and R5 are each H, halo, cyano, CH2OH, NO2, alkylthio, alkylsulfonyl, alkylsulfinyl, alkoxymethyl, CO2H, carbalkoxy, Ph, substd. Ph); R2=H, alkyl, PhCH2, Ph; n=1,2! were prepd. from 2-amino-5(6)-substd. cpd. with sulphonyl chloride or haloalkyl isothiocyanate in the presence of an acid acceptor base, water and a water miscible nonhydroxylic solvent at 0- 75≦̸C.