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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.
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Annear et al. (2025) studied this question.
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