C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 305/14 (2006.01) A61K 31/337 (2006.01) C07D 407/12 (2006.01) C07D 493/08 (2006.01)
Patent
CA 2155013
Taxane derivatives having alternative C2 substituent which is -OCOR31 wherein R31 is substituted phenyl and the substituent is selected from the group consisting of alkanoxy, protected hydroxy, halogen, alkyl, aryl, alkenyl, acyl, acyloxy, nitro, amino and amido. The taxane derivatives have the form of Image wherein X1 is -OX6, -SX7, or -NX8X9; X2 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; X3 and X4 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; X5 is -COX10, or -SO2X11; X6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxy protecting group; X7 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or sulfhydryl protecting group; X8 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or heterosubstituted alkyl, alkenyl, alkynyl, aryl or heteroaryl; X9 is an amino protecting group; X10 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, t-butoxy or heterosubstituted alkyl, alkenyl, alkynyl, aryl or heteroaryl; X11 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, -OX10, or -NX8X14; X14 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; R1 is hydrogen, hydroxy, protected hydroxy or together with R14 forms a carbonate; R2 is -OCOR31; R2a is hydrogen; R4 is hydrogen, together with R4a forms an oxo, oxirane or methylene, or together with R5a and the carbon atoms to which they are attached form an oxetane ring; R4a is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyano, hydroxy, -OCOR30, or together with R4 forms an oxo, oxirane or methylene; R5 is hydrogen or together with R5a forms an oxo, R5a is hydrogen, hydroxy, protected hydroxy, acyloxy, together with R5 forms an oxo, or together with R4 and the carbon atoms to which they are attached form an oxetane ring; R6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, hydroxy, protected hydroxy or together with R6a forms an oxo; R6a is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, hydroxy, protected hydroxy or together with R6 forms an oxo; R7 is hydrogen or together with R7a forms an oxo, R7a is halogen, hydroxy, or together with R7 forms an oxo; R9 together with R9a forms an oxo; R9a together with R9 forms an oxo; R10 is hydrogen; R10a is -OCOR29, hydroxy, or protected hydroxy; R14 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, hydroxy, protected hydroxy or together with R1 forms a carbonate; R14a is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; R29 and R30 are independently hydrogen, alkyl, alkenyl, alkynyl, monocyclic aryl or monocyclic heteroaryl; and R31 is substituted phenyl which is substituted with an alkyl, p-hydroxy, o-hydroxy, alkoxy, halogen, trifluoromethyl, protected hydroxy, aryl, alkenyl, acyl, acyloxy, nitro, amino, or amido substituent. The taxane derivatives are antileukemia and antitumor agents.
Holton Robert A.
Tao Chunlin
Florida State University
Smart & Biggar
LandOfFree
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