Expanded applicability of iridium(I) NHC/phosphine catalysts in hydrogen isotope exchange processes with pharmaceutically-relevant heterocycles

TETRAHEDRON

卷:71

Article

Atzrodt, Jens¹  Derdau, Volker¹  Kerr, William J.²  Reid, Marc²  Rojahn, Patrick¹  Weck, Remo¹ 

[1] Sanofi Aventis Deutschland GmbH, DSAR, Drug Disposit Isotope Chem & Metab Synth Ind Hoch, Frankfurt, Germany

[2] Univ Strathclyde, WestCHEM, Dept Pure & Appl Chem, Glasgow G1 1XL, Lanark, Scotland

关键词: Hydrogen isotope exchange;    Deuterium labelling;    Iridium catalysis;    N-Heterocyclic carbene;    Heterocycles;   

DOI  :  10.1016/j.tet.2015.02.029

来源: Elsevier

【 摘 要 】

An assessment of emerging C-H activation catalysts of the type [(COD)Ir(IMes)(PR3)]PF6 in the deuteration of N-heterocycles is divulged. Substrate scope, competition experiments and labelling of drug type molecules have revealed PR3=PPh3 provides a broadly more applicable and widely effective catalyst system compared to other available complexes in the present series. (C) 2015 Elsevier Ltd. All rights reserved.

【 授权许可】

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