One‐Pot Synthesis of Biheterocycles Based on Indole and Azole Scaffolds Using Tryptamines and 1,2‐Diaza‐1,3‐dienes as Building Blocks

Abstract

The rapid and expedient assembly of three new classes of biheterocycles of biological interest, viz. indole–imidazoles 4 , indole–pyrroles 6 and indole–triazoles 8 was accomplished using different combinations of tryptamines, 1,2‐diaza‐1,3‐dienes, aldehydes, and/or alkynes as readily available building blocks. Twenty‐six derivatives were thus prepared in excellent yields (up to 100 %). The products were screened for in‐vitro biological studies. Some of these revealed promising anticancer activity against MCF7 and Caco‐2 human tumor cell lines.