| 摘要 |
Aminomethyl-substituted benzo-cycloalkene or benzo-heterocyclic compounds (I) are new. Also new are tertiary alcohol intermediates (II). Bicyclic compounds of formula (I) and their salts are new. R1 = H, F, Cl, OH, 1-6C alkoxy, 3-7C cycloalkoxy, 1-6C alkyl, CH2F, CHF2 or CF3; R2 = H, F, Cl, 1-6C alkyl, CH2F, CHF2 or CF3; R3, R4 = H, F, Cl, OH, 1-6C alkoxy, 3-7C cycloalkoxy, 1-6C alkyl, CH2F, CHF2, CF3, aryloxy, aryl or heterocyclyl; R5, R6 = 1-6C alkyl, 3-7C cycloalkyl, (3-7C) cycloalkylmethyl, aryl, (1-5C alkyl)-aryl, heterocyclyl or (1-6C alkyl)-heterocyclyl; X = CH2, O, S, SO or SO2; n = 1-3; the dotted lines indicate that a double bond (endocyclic or exocyclic) is present in one of the the two indicated positions, the configuration being E or Z if the exocyclic double bond is present. Independent claims are included for: (i) the preparation of (I); and (ii) new tertiary alcohol intermediates of formula (II). R7 = R1 or R'1; R'1 = as R1, except that the value OH is replaced by OCH2Ph or OSiR10R11R12; R10 - R12 = 1-6C alkyl or Ph; R8/R9 = as R3/R4; or R'3/R'4; R'3/R'4 = as R3/R4, except that the value OH is replaced by OCH2Ph or OSiR10R11R12.
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