abstract |
A taxane derivative having the formula (3) wherein X1 is -OX6; X2 is hydrogen; X3 is C1-C6 alkyl, C2-C6 alkenyl, phenyl, furyl, thienyl or pyridyl; X4 is hydrogen; X5 is -CONX8X10; X6 is hydrogen; X8 is hydrogen, C1-C6 alkyl, benzyl or phenyl; X10 is C1-C6 alkyl, phenyl, benzyl or morpholino; R1 is hydroxy; R2 is hydroxy or -OCOR31; R2a is hydrogen; R4 together with R5a and the carbon atoms to which they are attached form an oxetane ring; R4a is hydroxy or -OCOR30; R5 is hydrogen; R6 is hydrogen; R6a is hydrogen; R7 is hydrogen; R7a is hydroxy; R9 is hydrogen or together with R9a forms an oxo; R9a is hydrogen, hydroxy, acyloxy, or together with R9 forms an oxo; R10 is hydrogen; R10a is -OCOR29 or hydroxy; R14 is hydrogen; R14a is hydrogen; R29 and R30 are independently C1-C6 alkyl; and R31 is phenyl. |