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US 4,857,653 AGranted
Process for the preparation of taxol and 10-deacetyltaxol
AssigneeRhone-Poulenc Sante
InventorsMichel Colin, Daniel Guenard, Francoise Gueritte-Voegelein, Pierre Potier
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Abstract
Taxol and 10-deacetyltaxol are prepared from a compound of formula: ##STR1## in which R' represents acetyl or 2,2,2-trichloroethoxycarbonyl radical, by removal of the t-butoxycarbonyl radical, benzoylation of the amine product obtained, and removal of the 2,2,2-trichloroethoxycarbonyl group(s).
Claims4
A process for the preparation of taxol or 10-deacetyltaxol, and their 2'S, 3'R isomers which comprises reacting halotrialkylsilane with a compound of formula:
- ##STR9## in which R' represents acetyl or 2,2,2-trichloroethoxycarbonyl, in an organic solvent at about 0.degree. C. to produce a product of formula:
- ##STR10## in which R' is as defined above, and reacting the said product with benzoyl chloride in the presence of an acid acceptor to produce a product of formula:
- ##STR11## in which R' is as defined above, and then reacting this product with zinc in acetic acid to produce taxol, when R' in the starting material is acetyl, or 10-deacetyltaxol, when R' in the starting material is 2,2,2-trichloroethoxycarbonyl.
Dependencies are inferred from the claim text.