Aao. Sarhan et al., SYNTHESIS AND REACTIONS OF NEW 4-CHLORO-2-METHYLPYRIMIDINO[4',5' 4,5]THIAZOLO[3,2-A]-BENZIMIDAZOLES/, Monatshefte fuer Chemie, 128(11), 1997, pp. 1133-1141
4-Chloro-2-methylpyrimidino [4',5':4,5]thiazolo[3,2-a]benzimidazole (3
) was prepared by chlorination of 2 which could also be converted dire
ctly to 2-methylpyrimidino [4',5':4,5]- thiazolo[3,2-a] benzimidazol-4
-thiol (4). Nucleophilic substitution of 3 with alcohols, phenols, pri
mary amines, secondary amines, sodium azide, and mercaptoacetic acid g
ave the corresponding derivatives. The thiol derivative 4 was reacted
with alkyl/aralkyl halides, phenacyl bromide derivatives, bromoacetone
, chloroanilides, bromomalonic ester, and ethyl bromoacetate to afford
compounds of potential pharmacological interest.