Expedient synthesis of mequitazine an antihistaminic drug by palladium catalyzed allylic alkylation of sodium phenothiazinate

  • Chem Pharm Bull (Tokyo). 2009 Nov;57(11):1300-2. doi: 10.1248/cpb.57.1300.
Vanessa Gonnot  1 ,  Marc Nicolas ,  Charles Mioskowski ,  Rachid Baati
Affiliations
  • 1. Faculty of Pharmacy, University of Strasbourg, CNRS-UMR 7199, 74 route du Rhin, 67401 Illkirch, France.
PMID: 19881287 DOI: 10.1248/cpb.57.1300
Abstract

A short and straightforward synthesis of the antihistaminic drug mequitazine is reported, based on an efficient palladium catalyzed allylic alkylation of 1-aza-bicyclo[2.2.2]oct-2-en-3-ylmethyl acetate using sodium phenothiazinate in mild conditions.

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