Patent ID: 6011056
Filing Date: 2000-01-04
Classification: C07C,C07D,C07F

Abstract:
A taxane having the formula ##STR31## 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 --COX.sub.10, --COOX.sub.10, --COSX.sub.10, --CONX.sub.8 X.sub.10, or --SO.sub.2 X.sub.11 ;X.sub.6 is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxy protecting group;X.sub.7 is substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, or sulfhydryl protecting group;X.sub.8 is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl;X.sub.9 is an amino protecting group;X.sub.10 is substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl;X.sub.11 is substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, --OX.sub.10, or --NX.sub.8 X.sub.14 ;X.sub.14 is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl;R.sub.1 is hydroxy, protected hydroxy or together with R.sub.14 forms a carbonate;R.sub.2 is hydroxy or --OCOR.sub.31 ;R.sub.4a is hydrogen, or substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyano, hydroxy, or --OCOR.sub.30 ;R.sub.7a is hydrogen, halogen, or --OR.sub.28 ;R.sub.9a is hydrogen, .beta.-hydroxy, .beta.-protected hydroxy or acyloxy;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, hydroxy, protected hydroxy or together with R.sub.1 forms a carbonate;R.sub.28 is hydrogen, acyl, or hydroxy protecting group; 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.