A general and efficient route to 6??methyl??pyrazin??2??yl??amines: Alkylation of 2, 6??dichloropyrazine via malonate derivatives

…, ME Giles, Z Patel, JT Singleton

Index: Colbon, Paul J. J.; Foster, Alison C.; Giles, Melvyn E.; Patel, Zakariya; Singleton, John T. Journal of Heterocyclic Chemistry, 2008 , vol. 45, # 5 p. 1451 - 1456

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Citation Number: 7

Abstract

We recently required a convenient synthesis of 6-methyl-pyrazin-2-yl-amine 1, which was an important intermediate in the synthesis of several compounds within our drug development program. A number of routes to 1 have been described in the literature but none are particularly efficient or amenable to large-scale manufacture [1-3]. For example, a one-step procedure starting from readily available 2-amino-6-chloropyrazine had been employed ...