合成路线1

The reaction of epothilone B (I) with MCPBA in dichloromethane gives the N-oxide (II), which is treated with trifluoroacetic anhydride and 2,6-lutidine in dichloromethane at 70 C in a sealed tube to yield the hydroxymethyl derivative (epothilone F) (III). The reaction of (III) with diphenylphosphoryl azide (DPA) and DBU in THF affords the azidomethyl compound (IV), which is reduced with PMe3 in THF or with H2 and Lindlar catalyst in ethanol to provide the target amino epothilone. Alternatively, the hydroxymethyl derivative (epothilone F) (III) can be obtained by biochemical hydroxylation of epothilone B (I) with Actinomyces sp. strain PTA-XXX.