Patent ID: 6965034
Filing Date: 2005-11-15
Classification: A61K,C07C,C07D,C07F

Abstract:
1. A process of making a desoxyepothilone comprising: (a) reacting a desoxyepothilone precursor having the structure:  with a macrolactonization reagent, wherein the macrolactonization reagent is selected from the group consisting of acetic anhydride, pentafluorophenol, 2,4-dichlorobenzoyl chloride, and 2.4,6-trichlorobenzoyl chloride, to generate a desoxyepothilone having the structure: wherein R, R R″ is —CY═CHX, or H, linear or branched chain alkyl, phenyl, 2-methyl-1,3-thiazol-4-yl, 2-furanyl, 3-furanyl, 4-furanyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, imidazolyl, 2-methyl-1,3-oxazol-4-yl, 3-indolyl or 6-indolyl; Y is H or linear or branched chain alkyl; and X is H, linear or branched chain alkyl, phenyl, 2-methyl-1,3-thiazol-4-yl, 2-furanyl, 3-furanyl, 4-furanyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, imidazolyl, 2-methyl-1,3-oxazol-4-yl, 3-indolyl or 6-indolyl; wherein Y is H or linear or branched chain alkyl; R R n is 2or 3.