Patent ID: 6965034

Claim:
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 0 and R′ are independently H, linear or branched chain alkyl, optionally substituted by hydroxy, OR 3 , alkoxy, carboxy, carboxaldehyde, linear or branched alkyl or cyclic acetal, fluorine, NR 1 R 2 , N-hydroximino, or N-alkoxyimino, wherein R 1 and R 2 are independently H, phenyl, benzyl, linear or branched chain alkyl; and R 3 is hydrogen, substituted or unsubstituted trialkylsilyl, dialkylarylsilyl, alkyldiarylsilyl, or triarylsilyl; 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 A is hydrogen or a linear or branched alkyl, substituted or unsubstituted alkoxyalkyl, substituted or unsubstituted alkoxycarbonyl, substituted or unsubstituted aryloxyalkyl, trialkylsilyl, aryldialkylsilyl, diarylalkylsilyl, triarylsilyl, linear or branched acyl, substituted or unsubstituted aroyl or benzoyl; R B is hydrogen, substituted or unsubstituted alkoxycarbonyl, t-butyloxycarbonyl, amyloxycarbonyl, (trialkylsilyl)alkyloxycarbonyl, (dialkylarylsilyl)alkoxycarbonyl, benzyl, trialkylsilyl, dialkylarylsilyl, alkyldiarylsilyl, triarylsilyl, a linear or branched acyl, or substituted or unsubstituted aroyl or benzoyl; and n is 2or 3.