Nonchromatographic isolation of 2-Alkyl-2H-1,2,3-triazoles in the synthesis of NK3 receptor antagonists

Abstract

A nonchromatographic isolation of a 2-alkyl-2H-triazole from a 1:1 mixture with the corresponding 1-alkyl-1H isomer was developed in a scalable synthesis of a synthetic intermediate for NK3 receptor antagonists. Based on the fundamental nucleophilicity difference in the isomeric triazoles, this method could be used as a general tactic in the isolation of 2H-triazoles. © 2010 American Chemical Society.