Photocatalytic N-Methylation of Amines over Pd/TiO2 for the Functionalization of Heterocycles and Pharmaceutical Intermediates

Papers published
Lyuming Wang, Kellie Jenkinson, Andrew E. H. Wheatley, Keiko Kuwata, Susumu Saito, and Hiroshi Naka, ACS Sustainable Chem. Eng., Just Accepted Manuscript DOI: 10.1021/acssuschemeng.8b03855
  • Amines in heteroaromatic systems and pharmaceutical intermediates were functionalized through N-methylation with methanol using a palladium-loaded titanium dioxide (Pd/TiO2) photocatalyst. This method provides access to a series of tertiary N-methylamines bearing N-, O-, and/or S-containing heteroaromatic functionalities from primary/secondary amines and methanol under mild reaction conditions. Facile syntheses of several pharmaceuticals containing N-methyl or ethyl groups, as well as related deuterated drugs, was achieved through the late-stage functionalization of amines.

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