The design and synthesis of a novel α-alkynylated biotin scaffold for use in heterobifunctional molecular probes

Abstract

Herein, we present a practical approach to the design and synthesis of an alkyne-functionalized biotin derivative. This compound can be utilized as a precursor for multifunctional molecular probes that contain both biotin and a desired synthetic fragment while preserving biotin's carboxylic acid moiety. Furthermore, we have demonstrated the applicability of this precursor to molecular probe design by synthesizing a modular thalidomide-biotin conjugate using copper-catalyzed azide-alkyne cycloaddition (CuAAC) as the key step.