An efficient synthesis of mequitazine

Y Guminski, V Fabre, P Lesimple…

Index: Guminski, Yves; Fabre, Valerie; Lesimple, Patrick; Imbert, Thierry Organic Preparations and Procedures International, 1999 , vol. 31, # 3 p. 319 - 323

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Citation Number: 4

Abstract

Mequitazine (l), a phenothiazine quinuclidine derivative known for more than two decades exhibits potent antihistamine properties and is the active constituent of some pharmaceuticals. The previously described synthesis in a patent is not satisfactory, leading to poor yields.'The strategy involves the preparation of the 3-hydroxymethyl quinuclidine (6) which was condensed via its chloro derivative with phenothiazine. The original six-step ...