Functionalization of NH-unsubstituted androstano[17,16-d]pyrazoles. Synthesis of 2-arylamino-2-thioxoacetylandrostano[17,16-d]pyrazoles

Abstract

An approach to the synthesis of earlier unknown androstano[17,16-d]pyrazoles containing a monothiooxamide fragment at the nitrogen atom of the pyrazole ring has been suggested. The method is based on the reaction of NH-unsubstituted androstano[17,16-d]pyrazole with chloroacetyl chloride with subsequent involvement of the obtained N-chloroacetylpyrazole into the reaction with elementary sulfur in the presence of aromatic amines. The synthesized androstano[17,16-d]pyrazoles containing a monothiooxamide fragment at the nitrogen atom of the pyrazole ring exhibit high antiparasitic activity.