Patent ID: 6335362
Filing Date: 2002-01-01
Classification: C07C,C07D,C07F

Abstract:
A taxane having the formula wherein X1 is â€”OX6, â€”SX7, or â€”NX8X9; X2 is hydrogen; substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl or alkynyl; or substituted or unsubstituted aryl or heteroaryl; X3 is substituted or unsubstituted, straight or branched chain alkyl, said alkyl being substituted methyl or comprising at least two carbon atoms in the principal chain; X5 is â€”COX10, â€”COOX10, â€”COSX10, â€”CONX8X10, or â€”SO2X11; X6 is hydrogen; substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl or alkynyl; or substituted or unsubstituted aryl or heteroaryl; X7 is substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl, or alkynyl; substituted or unsubstituted aryl or heteroaryl; or sulfhydryl protecting group; X8 is hydrogen; substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl or alkynyl; substituted or unsubstituted aryl or heteroaryl; or heterosubstituted alkyl, alkenyl, alkynyl, aryl or heteroaryl; X9 is an amino protecting group; X10 is substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl or alkynyl; substituted or unsubstituted aryl or heteroaryl; or heterosubstituted alkyl, alkenyl, alkynyl, aryl or heteroaryl; X11 is substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl or alkynyl; substituted or unsubstituted aryl or heteroaryl; â€”OX10; or â€”NX8X14; X14 is hydrogen; substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl or alkynyl; or substituted or unsubstituted aryl or heteroaryl; R1 is hydroxy, protected hydroxy or together with R14 forms a carbonate; R2 is hydroxy or â€”OCOR31; R4a is hydrogen; substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl or alkynyl; or substituted or unsubstituted aryl or heteroaryl; cyano; hydroxy; or â€”OCOR30; R7a is hydrogen, halogen, or â€”OR28; R9 is hydrogen or together with R9a forms an oxo; R9a is hydrogen, hydroxy, protected hydroxy, acyloxy, or together with R9 forms an oxo; R10 is hydrogen or together with R10a forms an oxo; R10a is hydrogen, â€”OCOR29, hydroxy, or protected hydroxy, or together with R10 forms an oxo; R14 is hydrogen, hydroxy, protected hydroxy or together with R1 forms a carbonate; R28 is hydrogen, acyl, or hydroxy protecting group; and R29, R30 and R31 are independently hydrogen; substituted, unsubstituted, straight, branched chain or cyclic alkyl; substituted, unsubstituted, straight or branched chain alkenyl or alkynyl; or substituted or unsubstituted monocyclic aryl or monocyclic heteroaryl.