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 ...
