| 摘要 |
C-21 Modified epothilone derivatives (I) are new. C-21 Modified epothilone derivatives of formula (I) are new. P-Q = C=C or an epoxide; G = a group of formula (i) or (ii); R = H or optionally substituted alkyl; R<1> = a group of formula (iii)-(viii); R<2> = a group of formula (ix); G<1> = H, halo, CN or optionally substituted alkyl; G<2> = H or optionally substituted alkyl; G<3> = O, S or NZ<1>; G<4> = H, optionally substituted alkyl, OZ<2>, NZ<2>Z<3>, Z<2>C=O, Z<4>SO2 or optionally substituted glycosyl; G<5> = halo, N3, NCS, SH, CN, NC, N(Z<1>)3<+> or heteroaryl; G<6> = H, optionally substituted alkyl, CF3, OZ<5>, SZ<5> or NZ<5>Z<6>; G<7> = CZ<7> or N; G<8> = H, halo, optionally substituted alkyl, OZ<10>, SZ<10> or NZ<10>Z<11>; G<9> = O, S, NH-NH or N=N; G<10> = N or CZ<12>; G<11> = NH2, alkyl or aryl (all optionally substituted); Z<1>, Z<6>, Z<9>, Z<11> = H, optionally substituted alkyl or optionally substituted acyl; Z<2> = H, optionally substituted alkyl or optionally substituted acyl or heterocyclyl; Z<3>, Z<5>, Z<8>, Z<10> = H, alkyl, acyl or aryl (all optionally substituted); Z<4> = optionally substituted alkyl, optionally substituted aryl or heterocyclyl; Z<7> = H, halo, optionally substituted alkyl, optionally substituted aryl, OZ<8>, SZ<8> or NZ<8>Z<9> and Z<12> = H, halo, optionally substituted alkyl or optionally substituted aryl; provided that when R<1> is (iii), G<1> and G<2> cannot be H, G<3> is not O and G<4> is not H or Z<2>C=O. Z = CO. An Independent claim is included for the preparation of a compound of formula (Ia).
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