A general approach to 2-substituted indoles

ORGN 75

Jacqueline H. Smitrovich, Chuanxing Qu, Ian W. Davies, and Dave Hughes. Department of Process Research, Merck Research Laboratories, P.O.Box 2000, Rahway, NJ 07065-0900
2-Substituted indoles are privileged structures of established medicinal chemistry value. Potential therapeutic targets include GnRH receptor antagonists and KDR kinase inhibitors. Synthesis of this class of compounds generally relies on a cross-coupling reaction between an appropriately functionalized 2-substituted indole and an aromatic partner. We are investigating alternative strategies to access these important targets that would obviate the need for both functionalization of the coupling partners and indole protection. Details of these current studies will be unveiled.
 

Process R&D
1:00 PM-5:00 PM, Sunday, September 7, 2003 Sheraton New York -- Royal Ballroom B, Oral

Division of Organic Chemistry
The 226th ACS National Meeting, New York, NY, September 7-11, 2003