The synthesis of [1-14 C]2-(1H-tetrazol-5-yl)acetic acid

Abstract

Tetrazoles are a common heterocyclic functionality in many biologically active molecules. [1-¹⁴ C]2-(1H-Tetrazol-5-yl)acetic acid was required as an intermediate in the synthesis of a development candidate as part of a discovery phase program to complete metabolic profiling studies. [1-¹⁴ C]2-(1H-Tetrazol-5-yl)acetic acid was prepared in 4 steps overall and in 3 radiochemical steps from K¹⁴ CN in an overall 32% radiochemical yield.

Keywords: [1-14C]2-(1H-tetrazol-5-yl)acetic acid; carbon-14; radiolabeled; tetrazoles.