| 摘要 |
<p>A new process and intermediates for preparing 1,4-benzodiazepines of formula (I) is disclosed: wherein, R<1> is H, OH, Br, I, NR<5>R<6>, CO2R<7>, CF3SO3, C1-4alkoxy, or (4,4'-bipiperidinyl) carbonyl; R<2> is alkyl, optionally substituted by CO2R<7> or CONR<5>R<6>; R<3> and R<3'> are independently H, Ar or C1-6 alkyl optionally substituted by OH, NO2, NH2, NR<5>R<6>, halogen, CO2R<7>, CONR<5>R<6> or Ar, or together R<3> and R<3'> are =O; R<4> is H or C1-4 alkyl, optionally substituted by OH, NO2, NH2, NR<5>R<6>, halogen, CO2R<7>, CONR<5>R<6>, or Ar; R<5> and R<6> are independently H, Ar, C1-6alkyl, HCO, C1-6alkyl-CO, Ar-CO, C1-6alkyl-SO2, or Ar-SO2; and R<7> is a carboxylic acid protecting group.</p> |
