Patent ID: 8299266
Filing Date: 2012-10-30
Classification: A61K,A61P,C07D,C07K

Abstract:
1. A process for making a compound having the formula G, or a pharmaceutically-acceptable salt thereof, wherein R Z Z R R R R R (i) preparing an epi-epothilone intermediate compound having the formula (A.1), by reacting a compound having the formula (C), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 12 , R 13 , Z 1 and Z 2 are as described above, with at least one halogenating agent to provide compounds having the formula (B.1) and/or (B.2), wherein Y is halogen and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 12 , R 13 , Z 1 and Z 2 are as described above followed by treatment of compounds (B.1) and/or (B.2) with base to provide the compound of formula A.1; (ii) treating the epi-epothilone intermediate of formula (A.1) with an azide donor in an alcohol solvent to provide azido-alcohols of formula (E.1) and (E.2), and (iii) treating the intermediate compounds provided by step (ii) with an azide reducing agent in a polar solvent to provide the compounds of formula (G).