| 摘要 |
Taxane derivatives of the formula (I) are new. R1 = phenyl or p-nitrophenyl, R3 = furyl or thienyl; T1 = H, a hydroxy-protecting gp. or -COT2, T2 = H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl or monocyclic aryl; Ac = acetyl; E1,E2 = H or a hydroxy-protecting gp.; or COGCOR'. G is ethylene, propylene, CH=CH, 1,2-cyclohexane or 1,2-phenylene; R1 is OH base, NR2R3, OR3, SR3, OCH2CONR7, or OH; R2 is H or CH3; R3 is (CH2)nFR6R7 or (CH2)nN(+)R6R7R8X(-); n is 1-3;R4 is H or 1-4C alkyl; R6 is H, 1-4C alkyl, benzyl, hydroxyethyl, CH2CO2H or dimethylaminoethyl;R6 and R7 are each CH3, C2H5 or benzyl; R8 is CH3, C2H5 or benzyl; X(-) is a halide; base is NH3, (HOC2H4)N, N(CH3)3, CH3N(C2H4OH)2, NH2(CH2)6NH2, N-methylglucamine, NaOH or KOH. |
