Patent ID: 7470792

Claim:
A process for the preparation of epothilone derivatives of formula 9: R1 is methyl; R2 is an unsubstituted or substituted aryl; an unsubstituted or substituted heteroaryl; or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus; comprising the steps of: a) reacting a compound of formula 1: wherein R2 has the meanings given above; wherein a mesylate group of the compound of formula 1 may be replaced with a tosylate group; and is an alcohol protecting group; with a compound of formula 2: in the presence of a Lewis acid and addition of a base in an inert solvent to yield a compound of formula 3: wherein R2 and have the above given meanings and wherein a mesylate group of the compound of formula 3 may be replaced with a tosylate group; b) the reacting compound of formula 3 in the presence of a silyl-ether forming compound to produce the compound of formula 4: wherein R2 and have the meanings given above and wherein a mesylate group of the compound of formula 4 may be replaced with a tosylate group; c) converting the compound of formula 4 to produce a compound of formula 5: wherein R2 and have the meanings given above and wherein the mesylate group of the compound of formula 5 may be replaced with a tosylate group; d) reacting compounds of above formula 5 with a reducing reagent in an inert solvent to yield a compound of formula 6: wherein R2 and the above have given meanings; e) hydrolysing the compound of formula 6, to produce a compound of formula 7: wherein R2 and have the above given meanings; f) macrolactonizing a compound of formula 7, to produce the epothilone derivative of formula 8: wherein R2 and have has the above defined meanings; and g) treating the compound of formula 8 with HF·pyridine in an inert solvent to produce the epothilone derivatives of formula 9.