| 摘要 |
Preparing 3-{3-[(3,4-dimethoxy-bicyclo[4.2.0]octa-1(6),2,4-trien-7-yl methyl)-methyl-amino]-propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-benzo[ d]azepin-2-one (VIII) comprises: reacting 3,4-dimethoxy-bicyclo[4.2.0 ]octa-1(6),2,4-triene-7-carbonitrile (II) and 7,8-dimethoxy-3-(3-methylamino-propyl)-1,3,4,5-tetrahydro-benzo[d]aze pin-2-one (IX) in the presence of lanthanide in a solvent to obtain N-[3-(7,8-dimethoxy-2-oxo-1,2,4,5-tetrahydro-benzo[d]azepin-3-yl)-pro pyl]-3,4-dimethoxy-N-methyl-bicyclo[4.2.0]octa-1(6),2,4-triene-7-carb oxamidine (X); and transforming (X) by the action of a hydride donor. Preparing 3-{3-[(3,4-dimethoxy-bicyclo[4.2.0]octa-1(6),2,4-trien-7-yl methyl)-methyl-amino]-propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-benzo[ d]azepin-2-one (VIII) or its racemic form or optically active form comprises: reacting 3,4-dimethoxy-bicyclo[4.2.0]octa-1(6),2,4-triene- 7-carbonitrile (II) and 7,8-dimethoxy-3-(3-methylamino-propyl)-1,3,4, 5-tetrahydro-benzo[d]azepin-2-one (IX) in the presence of transition metal or lanthanide in a solvent to obtain N-[3-(7,8-dimethoxy-2-oxo- 1,2,4,5-tetrahydro-benzo[d]azepin-3-yl)-propyl]-3,4-dimethoxy-N-methy l-bicyclo[4.2.0]octa-1(6),2,4-triene-7-carboxamidine (X); and transforming (X) by the action of a hydride donor. An INDEPENDENT CLAIM is included for N-[3-(7,8-dimethoxy-2-oxo-1,2,4,5-tetrahydro-be nzo[d]azepin-3-yl)-propyl]-3,4-dimethoxy-N-methyl-bicyclo[4.2.0]octa- 1(6),2,4-triene-7-carboxamidine (X). - ACTIVITY : Cardiant; Vasotropic; Antianginal; Antiarrhythmic. - MECHANISM OF ACTION : None given. |
