Synthesis of deuterium-labelled drugs by hydrogen-deuterium (H-D) exchange using heterogeneous catalysis

作者: Nkaelang Modutlwa , Tomohiro Maegawa , Yasunari Monguchi , Hironao Sajiki

DOI: 10.1002/JLCR.1848

关键词:

摘要: Multi-deuterium incorporations into drugs, such as theophylline, caffeine, valpromide, phenytoin, and trimethoprim, were post-synthetically achieved by Pd/C-, Pt/C-, or/and Rh/C-catalyzed hydrogen–deuterium exchange reactions under neutral conditions using deuterium oxide the source in presence of hydrogen gas. The present study offers facile convenient methods for preparation highly deuterated medicines, which are expected to be used long-lasting medicines well internal standards metabolic studies quantitative analyses parent drugs.

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