Novel Synthesis and Biological Activity of 2-Substituted Derivatives of 3-Cyano-4-imino-2-methylthio-8-methoxy-4H-pyrimido[2,1-b][1,3]benzothiaz ole and 3-Amino-4-imino-8-methoxy-2H-pyrazolo[3 ',4 ':4,5]pyrimido[2,1-b][1,3]benzothiazole

[摘要]：2-Amino-6-methoxybenzothiazole 1 on reaction with bis(methylthio) methylene malononitrile 2 in the presence of dimethyl formamide and catalytic amount of anhydrous potassium carbonate afforded 3-cyano-4-imino-8-methoxy-4H-pyrimido[2,1-b][1,3]benzothiazole 3. Under similar experimental conditions, compound 3 on treatment independently with arylamines/heterylamines/phenols/compounds containing active methylene group yielded corresponding 2-substituted derivatives of compound 3 (4(a-d), 5(a-c), 6(a-e), and 7(a-e)). Similarly, novel heterocyclic compounds, 3-amino-4-imino-8-methoxy-2H 8(a)/aryl 8(b-c)/heteryl 8(d-f)/pyrazolo[3',4':4,5]pyrimido[2,1-b][1,3]benzothiazoles, were prepared by heating compound 3 independently with hydrazine hydrate/arylhydrazines/heterylhydrazines, respectively. All these newly synthesized compounds were screened for antimicrobial activity.

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