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Synthesis of deuterium‐labelled drugs by hydrogen–deuterium (H–D) exchange using heterogeneous catalysis
Author(s) -
Modutlwa Nkaelang,
Maegawa Tomohiro,
Monguchi Yasunari,
Sajiki Hironao
Publication year - 2010
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1848
Subject(s) - chemistry , deuterium , hydrogen–deuterium exchange , hydrogen , catalysis , theophylline , organic chemistry , pharmacology , medicine , physics , quantum mechanics
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 as the deuterium source in the presence of hydrogen gas. The present study offers facile and convenient methods for the preparation of highly deuterated medicines, which are expected to be used as long‐lasting medicines as well as internal standards for metabolic studies and for the quantitative analyses of the parent drugs.