Patent ID: 6018073
Filing Date: 2000-01-25
Classification: C07D

Abstract:
A taxane having the formula ##STR145## wherein X.sub.1 is --OX.sub.6, --SX.sub.7, or --NX.sub.8 X.sub.9 ;X.sub.2 is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl;X.sub.3 and X.sub.4 are independently hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl or heteroaryl;X.sub.5 is --COOX.sub.10 ;X.sub.6 is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or hydroxy protecting group, or a functional group which increases the water solubility of the taxane derivative;X.sub.7 is substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or sulfhydryl protecting group;X.sub.8 is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or heterosubstituted alkyl, alkenyl, alkynyl, aryl or heteroaryl;X.sub.9 is an amino protecting group;X.sub.10 is substituted or unsubstituted alkyl, alkenyl or aryl;R.sub.1 is hydroxy, protected hydroxy or together with R.sub.14 forms a carbonate;R.sub.2 is hydrogen, hydroxy, --OCOR.sub.31, or together with R.sub.2a forms an oxo;R.sub.2a is hydrogen or taken together with R.sub.2 forms an oxo;R.sub.4 is hydrogen, or together with R.sub.4a forms an oxo, oxirane or methylene;R.sub.4a is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or cyano, hydroxy, --OCOR.sub.30, or together with R.sub.4 forms an oxo, oxirane or methylene;R.sub.5 is hydrogen or together with R.sub.5a forms an oxo;R.sub.5a is hydrogen, hydroxy, protected hydroxy, acyloxy, or together with R.sub.5 forms an oxo;R.sub.6 is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or hydroxy, protected hydroxy or together with R.sub.6a forms an oxo;R.sub.6a is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or hydroxy, protected hydroxy or together with R.sub.6a forms an oxo;R.sub.7 is hydrogen or together with R.sub.7a forms an oxo;R.sub.7a is hydrogen, halogen, protected hydroxy, --OR.sub.28, or together with R.sub.7 forms an oxo;R.sub.9 is hydrogen or together with R.sub.9a forms an oxo;R.sub.9a is hydrogen, hydroxy, protected hydroxy, acyloxy, or together with R.sub.9 forms an oxo;R.sub.10 is hydrogen or together with R.sub.10a forms an oxo;R.sub.10a is hydrogen, --OCOR.sub.29, hydroxy, or protected hydroxy, or together with R.sub.10 forms an oxo;R.sub.14 is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or hydroxy, protected hydroxy or together with R.sub.1 forms a carbonate;R.sub.14a is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl;R.sub.28 is hydrogen, acyl, hydroxy protecting group or a functional group which increases the solubility of the taxane derivative; andR.sub.29, R.sub.30, and R.sub.31 are independently hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, monocyclic aryl or monocyclic heteroaryl.