Synlett

A Facile Synthesis of 5-Halopyrimidine-4-Carboxylic Acid Esters via a Minisci Reaction

CF Regan, F Pierre, MK Schwaebe, M Haddach…

Index: Regan, Collin F.; Pierre, Fabrice; Schwaebe, Michael K.; Haddach, Mustapha; Jung, Michael E.; Ryckman, David M. Synlett, 2012 , # 3 p. 443 - 447

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Abstract

Abstract This paper reports the synthesis of various 5-halopyrimidine-4-carboxylic acid esters via the Minisci homolytic alkoxycarbonylation of 5-halopyrimidines. The reaction was found to be highly regioselective, allowing the one-step synthesis of useful amounts (> 10 g) of ethyl 5-bromopyrimidine-4-carboxylate where other methods proved difficult. Ethyl 5- bromopyrimidine-4-carboxylate was used for the preparation of potent CK2 inhibitors ...