Tetrahedron Letters

First synthesis of 4-chloro-2, 2-difluoro [1, 3] dioxole [4, 5-c] pyridine

MP Catalani, A Paio, L Perugini

Index: Catalani, Maria Pia; Paio, Alfredo; Perugini, Lorenzo Tetrahedron Letters, 2010 , vol. 51, # 51 p. 6783 - 6785

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Abstract

The 2, 2-difluorobenzodioxole moiety has been introduced in medicinal chemistry research as a potential metabolically more stable derivative of the benzodioxole fragment. Herein we present, to the best of our knowledge, the first synthesis of 4-chloro-2, 2-difluoro [1, 3] dioxole [4, 5-c] pyridine, a 5-aza-derivative of the 2, 2-difluorobenzodioxole, from simple and cheap starting materials. The chlorine atom in position 4 could be useful for further ...