Improved Synthesis of Amino Acid and Dipeptide Chloromethyl Esters Using Bromochloromethane
- 6 January 2003
- journal article
- Published by Informa UK Limited in Synthetic Communications
- Vol. 33 (10), 1683-1693
- https://doi.org/10.1081/scc-120018930
Abstract
Peptide chloromethyl esters are important compounds in prodrug synthesis. A simple, mild and efficient method for the synthesis of chloromethyl esters of N-blocked amino acids and dipeptides using exclusively bromochloromethane is reported. These N-blocked amino acid and dipeptide chloromethyl esters react readily with the carboxylic acid group of aspirin and with the sulfonamido group of the antimalarial sulfamethazine, to give the corresponding prodrugsKeywords
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