General method of obtaining deuterium-labeled heterocyclic compounds using neutral D2O with heterogeneous Pd/C |
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Authors: | Hiroyoshi Esaki Shino Sakai Yasunari Monguchi |
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Affiliation: | a Laboratory of Medicinal Chemistry, Gifu Pharmaceutical University, 5-6-1 Mitahora-higashi, Gifu 502-8585, Japan b Chemical Products Research Laboratories, Wako Pure Chemical Industries, Ltd, 1633 Matoba, Kawagoe 350-1101, Japan |
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Abstract: | A protocol of a versatile H-D exchange reaction of heterocyclic compounds catalyzed by heterogeneous Pd/C in D2O is described. The reaction of various nitrogen-containing heterocycles with 10% Pd/C (10 wt % of the substrate) under hydrogen atmosphere in D2O as a deuterium source at 110-180 °C for 24 h afforded the corresponding deuterated compounds with satisfactory efficiency of deuteration in moderate to excellent isolated yields. Furthermore, the Pd/C-H2-D2O system can be extended to the direct deuteration of biologically active compounds such as sulfamethazine, which is used as a synthetic antibacterial drug for fat stocks and would be applied as a general method for the preparation of the standard materials for the analysis of residual chemicals in foods and so on. |
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