A concise synthesis of the HCV protease inhibitor BILN 2061 and its P3 modified analogs

D Liu, J Dong, Y Yin, R Ma, Y Shi, H Wu…

Index: Liu, Dejun; Dong, Jingchao; Yin, Yunxing; Ma, Rujian; Shi, Yifeng; Wu, Hao; Chen, Shuhui; Li, Ge Chinese Journal of Chemistry, 2011 , vol. 29, # 7 p. 1489 - 1502

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Abstract

Abstract A concise synthesis of BILN 2061 was achieved through more efficient installation of P2 4-quinoline moiety via SN 2 displacement of the β-OBs group located on the 4- hydroxyl proline intermediate, which was prepared from 4-α-hydroxyl proline analog via Mitsunobu reaction with inversion of stereochemistry. In addition, a short and practical synthesis for P3 unit is also described herein. Final assembly of four fragments for BILN ...