Faucher Anne-Marie, Bailey Murray D, Beaulieu Pierre L, Brochu Christian, Duceppe Jean-Simon, Ferland Jean-Marie, Ghiro Elise, Gorys Vida, Halmos Ted, Kawai Stephen H, Poirier Martin, Simoneau Bruno, Tsantrizos Youla S, Llinàs-Brunet Montse
Chemistry Department, Boehringer Ingelheim (Canada) Ltd., Research and Development, 2100 Cunard Street, Laval, Québec, Canada H7S 2G5.
Org Lett. 2004 Aug 19;6(17):2901-4. doi: 10.1021/ol0489907.
The synthesis of BILN 2061, an NS3 protease inhibitor with proven antiviral effect in humans, was accomplished in a convergent manner from four building blocks. The procedure described here was suitable for the preparation of multigram quantities of BILN 2061 for preclinical pharmacological evaluation.
BILN 2061是一种在人体中已证实具有抗病毒作用的NS3蛋白酶抑制剂，它由四个构建模块以汇聚方式合成。本文所述方法适用于制备数克量的BILN 2061，用于临床前药理评估。
