摘要：

4-Chloro-2-methylpyrimidino[4<img src="/content/L677887724R74604/xxlarge8242.gif" alt="prime" align="BASELINE" border="0">,5<img src="/content/L677887724R74604/xxlarge8242.gif" alt="prime" align="BASELINE" border="0">:4,5]thiazolo[3,2-a]benzimidazole (3) was prepared by chlorination of2 which could also be converted directly to 2-methylpyrimidino[4<img src="/content/L677887724R74604/xxlarge8242.gif" alt="prime" align="BASELINE" border="0">,5<img src="/content/L677887724R74604/xxlarge8242.gif" alt="prime" align="BASELINE" border="0">:4,5]-thiazolo[3,2-a]benzimidazol-4-thiol (4). Nucleophilic substitution of3 with alcohols, phenols, primary amines, secondary amines, sodium azide, and mercaptoacetic acid gave the corresponding derivatives. The thiol derivative4 was reacted with alkyl/aralkyl halides, phenacyl bromide derivatives, bromoacetone, chloroanilides, bromomalonic ester, and ethyl bromoacetate to afford compounds of potential pharmacological interest.

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