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.