Hydrogen–Deuterium Exchange Reactions of Aromatic Compounds and Heterocycles by NaBD4‐Activated Rhodium,Platinum and Palladium Catalysts |
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| Authors: | Volker Derdau Dr. Jens Atzrodt Dr. Jochen Zimmermann Dr. Carsten Kroll Francois Brückner |
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| Affiliation: | Sanofi‐Aventis Deutschland GmbH, Isotope Chemistry & Metabolite Synthesis Frankfurt, Industriepark H?chst G876, 65926 Frankfurt am Main (Germany), Fax: (+49)?69 30517082 |
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| Abstract: | Conventional thermal and microwave conditions were compared for hydrogen–deuterium (H/D) exchange reactions of aminobenzoic acids catalysed by NaBD4‐activated Pd/C or RhCl3 with D2O as the deuterium source. We also investigated different NaBD4‐activated metal catalysts (including Pd/C, RhCl3 and Pt/C) under microwave conditions for an efficient H/D exchange of aromatic and heterocyclic compounds. Even higher deuterium incorporations were obtained for Pd/C and Pt/C catalyst mixtures due to the previously observed synergistic effect. Finally, we have applied these optimised conditions for one‐step syntheses of the MS standards of several pharmaceutically active compounds. |
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| Keywords: | C?H activation deuterium hydrogen– deuterium exchange microwave chemistry |
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