Drug Metabolism (Track)



AN EFFICIENT CATALYTIC SYSTEM FOR C-H ACTIVATION: A NOVEL AND PRACTICAL SYNTHESIS OF ANGIOTENSIN II RECEPTOR BLOCKERS

Masahiko Seki

Healthcare Business Division II, API Corporation, 2-3-4, Nihonbashi, Chuo-ku, Tokyo 103-0027, Japan


Abstract:


The C-H activation provided access to a wide variety of highly functionalized biaryls involving drugs and other commercially significant compounds. However the previous procedures need high loading of expensive catalysts which inevitably prevent their commercial application. We have developed a quite efficient catalytic system which required an unprecedentedly low catalyst loading. In this presentation will be presented the efficient protocol using a practical synthesis of an important class of pharmaceuticals, angiotensin II receptor blockers, as an example [1].





[1] (a) Seki, M. WO2011061996A1, 2010. (b) Seki, M. ACS Catal. 2011, 1, 607. (c) Seki. M.; Nagahama, M. J. Org. Chem. 2011, 76, 10198.