| 摘要 |
Mikanolide derivatives (I) (i.e. macrocyclic mono- or diepoxy dilactone compounds) (I) are new. Mikanolide derivatives of formula (I) and their salts are new. R1 = H, SR4 or NR4R5; R2 = SR6 or NR6R7 (both in alpha -configuration); R3 = OH, OC(O)R14, OSiR15R16R17, OC(O)OR18 or OC(O)NHR18; or R2 (in beta -configuration) + R3 = O of alpha , alpha -epoxide; R4 - R7 = alkyl, cycloalkyl, cycloalkylalkyl or hydroxyalkyl; or aryl or aralkyl (both optionally ring-substituted by one or more of alkyl, OH and alkoxy); and R5 and/or R7 = H; or NR4R5 and/or NR6R7 = 5-7 membered heterocycle in which the other members are CR8R9, NR10, O or S (provided that only one of O or S may be present); R8, R10 = H, alkyl, alkoxycarbonyl or aralkyl; R9 = H; or R8 + R9 = OCH2CH2O, provided that only one such group may be present in the heterocycle and that the carbon atoms to which the group is bonded carry H or alkyl groups; R14, R18 = alkyl, cycloalkyl or adamantyl; aryl, aralkyl, heteroaryl or heteroaralkyl (all optionally ring-substituted by one or more of halo, alkyl, haloalkyl, NO2, OH, alkoxy, alkylthio and phenyl); or R14 may also be a group such that R14COOH is a natural aminoacid (optionally in enantiomeric form); R15 - R17 = alkyl or phenyl; provided that if R2 R3 = O, then R1 is other than H.
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