Abbott Laboratories, GPRD Process Research and Development, Dept. R450, Bldg. R8, 1401 Sheridan Road, North Chicago, Illinois 60064, USA.
J Org Chem. 2009 Dec 18;74(24):9539-42. doi: 10.1021/jo901943s.
A five-step synthesis of a TRPV1 receptor antagonist 1 is described. The key step involves a novel palladium-catalyzed amidation reaction of 4-chloro-1-methylindazole 8 with the benzyl urea 9 to form the unsymmetrically substituted urea 1.
本文描述了 TRPV1 受体拮抗剂 1 的五步合成路线。关键步骤涉及新颖的钯催化 4-氯-1-甲基吲唑 8 与苄基脲 9 的酰胺化反应,形成不对称取代的脲 1。