Taxane derivatives and processes for the preparation thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 263/06 (2006.01) C07D 305/14 (2006.01) C07D 493/08 (2006.01)

Patent

CA 2676424

The present invention is directed to a process for the preparation of (4S,5R)-N-Boc-2-(2,4-dimethoxyphenyl)-4-isobutyl- 1-oxazolidine-5-carboxylic acid. This compound is useful as an intermediate for the synthesis of baccatine III and V derivatives substituted at the 13-position by a N-Boc-~- isobutyl-serinyl residue. Such compounds show anticancer activity.

La présente invention a pour objet un procédé de préparation d'acide (4S,5R)-N-boc-2-(2,4-diméthoxyphényl)-4-isobutyl-1-oxazolidine-5-carboxylique. Ce composé est utile comme intermédiaire pour la synthèse de baccatine III et de dérivés V substitués en position 13 par un résidu de N-boc-~- isobutyl-sérinyle. De tels composés exhibe une activité contre le cancer.

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