| 摘要 |
PROBLEM TO BE SOLVED: To obtain an intermediate useful for synthesizing an intermediate of benzo[b]azepin-2-one CCK antagonist. SOLUTION: A compound of formula I (X is phenyl, a 3-8C alkyl or the like; and Y1 and Y2 are each a halogen, nitro, amino or the like) and a compound of formula II (L is hydroxyl, chloro or the like) are allowed to react with each other in an organic solvent and the resultant reaction product is allowed to react with a base in an organic solvent to give the compound of formula III. Then, the compound of formula III is reduced with Raney nickel and a hydrogen source to prepare a synthetic intermediate for CCK antagonist represented by formula IV. The resultant compound of formula IV is racemic and includes 4 kinds of isomer comprising individually 2 kinds of the cis isomers and the trans isomers, respectively, but the content of the trans isomers are <=10 % of the reaction products in a preferred embodiment. The compound of formula III is a novel intermediate for synthesizing a compound of formula IV.
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