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

✍ Scribed by Paul J. J. Colbon; Alison C. Foster; Melvyn E. Giles; Zakariya Patel; John T. Singleton

• Publisher: Journal of Heterocyclic Chemistry
• Year: 2008
• Tongue: English
• Weight: 424 KB
• Volume: 45
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.5570450531

✦ Synopsis

Abstract

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We have developed a convenient two‐stage process for the synthesis of 6‐methylpyrazine‐2‐yl‐amines from commercially available materials. The procedure involves the synthesis of (6‐chloro‐pyrazin‐2‐yl)‐acetic acid via arylation of diethyl malonate and in situ hydrolysis/decarboxylation. A second decarboxylation takes place under the subsequent amination conditions allowing simple and efficient access to the intended pyrazines.