Abstract

This report describes an efficient and mild approach for the synthesis of Piperastrol and Enastron via a one-pot three-component cyclocondensation reaction employing ammonium sulfocyanate (NH4SCN) on gram scale in isopropyl alcohol–PEG 400 medium. In this reaction, ammonium sulfocyanate is not only the reacting component but also accelerates the rate of reaction to afford Biginelli compounds. High yields, short reaction time and easy workup procedure are the key advantages of the present protocol. Ammonium sulfocyanate is readily available, cheaper, safer and industrially acceptable inorganic salt.

Keywords: Enastron, piperastrol, catalyst free, ammonium sulfocyanate, biginelli reaction, anticancer.

Graphical Abstract