Process for preparing taxane derivatives

Details Process for preparing taxane derivatives Process for preparing taxane derivatives

1997-08-08

1999-02-09

Trinh, Ba K.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548216, 549510, 549511, C07D26304, C07D30514

Patent

active

058696806

ABSTRACT:
This invention relates to a method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III by means of an acid of general formula (VII), elimination of protection groupings of the ester obtained, and acylation of the amine function of the side chain. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 -CO--O- in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 and R.sub.4 may be the same or different and represent hydrogen, alkyl, alkenyl, aralkyl, aryl or alkoxy, and R.sub.5 is an alkyl radical substituted by one or more chlorine atoms (2,2,2-trichloroethyl, 2-trichloromethylisopropyl). ##STR1##

REFERENCES:
patent: 5015744 (1991-05-01), Holton
patent: 5136060 (1992-08-01), Holton
patent: 5175315 (1992-12-01), Holton
patent: 5319112 (1994-06-01), Kingston et al.
Gueritte-Voegelein et al., J. Med. Chem. vol. 34 (3):992-998 Mar. 1991.
Kingston et al., Stud. Org. Chem. (New Trends in Nat. Prod. Chem. 1986), vol. 26:219-235 1986.

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