| 摘要 |
8 beta -Substituted-11 beta -(p-substituted phenyl)-estra-2,3,5(10)-triene derivatives (I) are new. 8 beta -Substituted-11 beta -(p-substituted phenyl)-estra-2,3,5(10)-triene derivatives of formula (I) and their acid addition salts are new. R<2> = H, halo, R<18>, OR<18> or OSO2R<19>; R<18> = H, 1-6C alkyl (optionally containing 1 or 2 multiple bonds), up to 6C alkanoyl (optionally containing 1 or 2 multiple bonds), COPh or CF3; R<19> = NR<20>R<21>; R<20>, R<21> = H, 1-5C alkyl, COR<22>, optionally substituted (os) 3-7C cycloalkyl, os 4-15C cycloalkylalkyl, os aryl, os heteroaryl or os aralkyl; or NR<20>R<21> = 4-6C polymethyleneimino or morpholino; R<22> = os, optionally mono- or polyhalogenated, saturated or mono-, di- or triunsaturated 1-10C hydrocarbyl; R<3> = OR<1>8', OSO2R<19> or OCOR<22>; R<1>8' = as R<18>; or aryl, heteroaryl or aralkyl; R<6>, R<7> = H; R6' = H, OH or R<22>; R7', R<1>5', R<1>6' = H, halo, OR<18>, OSO2R<19> or OCOR<22>; R<8> = optionally mono- or polyhalogenated 1-5C alkyl, optionally mono- or polyhalogenated 2-5C alkenyl, ethynyl or prop-1-ynyl; X = direct bond, O or S; n = 1-12 (the corresponding alkylene group optionally being interrupted by 1-3 O, S or NMe); Y = NR<25>R<26>, CONR<25>R<26> or S(O)mR<27>; R<25>, R<26> = H, os, optionally mono- or polyhalogenated, saturated or mono-, di- or triunsaturated 1-10C hydrocarbyl, os 3-7C cycloalkyl, os 4-15C cycloalkylalkyl, os aryl, os heteroaryl or os aralkyl; or NR<25>R<26> = heterocycle (optionally containing a further O, S or N heteroatom and os by 1-4C alkyl); m = 0-2; R<27> = os, optionally mono- or polyhalogenated, saturated or mono-, di- or triunsaturated 1-10C hydrocarbyl, os 3-7C cycloalkyl, os 4-5C cycloalkylalkyl, os aryl, os heteroaryl or os aralkyl; R<14>-R<16> = H; or R<14> + R<15> or R<15> + R<16> = additional bond; R<17>, R<1>7' = H/H, H/halo, H/OCH2Ph, H/OSO2R<19>, R<18>/COR<22>, R<18>/OCOR<22>, OR<18>/R<18> or OR<18>/OCOR<22>; or R<17> + R<1>7' = =CR<23>R<24> or =O; R<23>, R<24> = H or halo.
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