An efficient, mild and solvent-free synthesis of benzene ring acylated harmalines

Abstract

A facile synthesis of a series of benzene ring acylated analogues of harmaline has been achieved by Friedel-Crafts acylation under solvent-free conditions at room temperature using acyl halides/acid anhydrides and AlCl 3. The reaction afforded 10- and 12-acyl analogues of harmaline in good yield, along with minor quantities of N-acyltryptamines and 8-acyl analogues of N-acyltryptamines.