Collin F. Regan, F. Pierre, M. Schwaebe
Feb 1, 2012
Citations
0
Influential Citations
4
Citations
Journal
Synlett
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 including CX-5011. This work represents an interesting application of radical chemistry for the preparation of pharmacologically active molecules.