| 摘要 |
The invention relates to a .beta.-lactam of the formula (see fig. I) wherein R1 and R3 are independently selected from phenyl, naphthyl, C6H5CHCH-, and (see fig. II) (see fig. III) or (see fig. IV) Q is CH3-, (CH3)3C-, CH3)-, Cl, Br, F, or NO2; and R2 is hydrogen or hydroxy protecting group. The .beta.-lactams are useful as intermediates in the preparation of a taxane derivative of the formula (see fig. IV) wherein R1 and R3 are independently selected from the group comprising phenyl, naphthalene, C6H5CHCH-, (see fig. V), (see fig. VI) and (see fig. VII) provided, however, R1 and R3 are not both phenyl; Q is CH3-, (CH3)3C-, CH3O-, Cl, Br, F, or NO2; Z is -OT1; T1 is hydrogen, hydroxyl protecting group, or -COT2; T2 is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or monocylic aryl; Ac is acetyl; and E1 and E2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
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