Practical synthesis of a vanilloid receptor-1 antagonist

…, C Bernard, T King, M Dilmeghani-Seran…

Index: Thiel, Oliver R.; Bernard, Charles; King, Tony; Dilmeghani-Seran, Mina; Bostick, Tracy; Larsen, Robert D.; Faul, Margaret M. Journal of Organic Chemistry, 2008 , vol. 73, # 9 p. 3508 - 3515

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Citation Number: 27

Abstract

Small molecule TRPV1 antagonists have been a recent focus in the search for pain treatment agents. We herein describe a practical and scalable synthesis of AMG 628 (1), a bis-substituted pyrimidine derivative that was identified as a highly efficacious agent, suitable for clinical development. Highlights of our approach include a practical route to a substituted benzothiazole, a scalable synthesis of an enantiopure piperazine fragment, ...

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