Development of an efficient, practical synthesis of a potent KDR kinase inhibitor

ORGN 521

Jeffrey T Kuethe, Audrey Wong, Jacqueline H. Smitrovich, Chuaxing Qu, Ian W. Davies, and David L. Hughes. Department of Process Research, Merck & Co., Inc, P.O. Box 2000, Rahway, NJ 07065
The evolution of a concise and efficient synthesis of a potent and selective KDR kinase inhibitor will be presented. The strategy centers on the construction of the indole ring rather than functionalization of a preformed indole core and allows for the preparation of the target compound from readily available bulk chemicals in 56% overall yield. Key aspects of the route selection and the final synthesis will be discussed.

 

Practical Synthesis and Total Synthesis of Complex Molecules
8:00 AM-12:00 PM, Wednesday, August 25, 2004 Pennsylvania Convention Center -- 201B, Oral

Division of Organic Chemistry

The 228th ACS National Meeting, in Philadelphia, PA, August 22-26, 2004