Novel Approach to Antihistamine-type Scaffolds
Gautam Panda describes the 1,6-aza-Michael addition of heterocyclic amines and amides to para-quinone methides.
Base-Mediated 1,6-Aza-Michael Addition of Heterocyclic Amines and Amides to para-Quinone Methides Leading to Meclizine-, Hydroxyzine- and Cetirizine-like Architectures: D. Roy, G. Panda
Synthesis 2019, DOI: 10.1055/s-0039-1690677
A number of drugs – including cetirizine and related antihistamine drugs – belong to the structural class of trisubstituted methanes, and specifically to that of diphenylmethanes having a heterocyclic amine attached to the bis-benzylic carbon. A conceptually new and convenient approach to these molecules has been recently developed by the group of Professor Gautam Panda from the CSIR-Central Drug Research Institute (Lucknow, India).
Professor Panda said: “Our group developed a 1,6-aza-Michael addition to synthesize meclizine-, hydroxyzine- and cetirizine-like architectures which may easily generate chemical libraries of antihistamines.”