| 摘要 |
NEW MATERIAL:The compound of formula I [A is halogen or lower alkoxy; R is H, 1-3C alkyl, etc.; Y is piperidyl, group of formula II (R<1> and R<2> are 1-3C alkyl), etc.; when A is halogen, Y is not 1-piperazyl] and its salt. EXAMPLE:8-Chloro-4-dimethylaminomethyl-2,3-dihydro-1-benzoxepin. USE:Remedy and amelioration agent for symptoms caused by the cerebral organic disorder such as the sequela of cerebral infarction or pathergasia such as ademonia, etc. PREPARATION:The objective compound can be prepared by (1) reacting the phenol derivative of formula III with gamma-butyrolactone in the presence of a base, (2) reducing the resultant 4-phenoxybutyric acid derivative with an acid to obtain 1-benzoxepin derivative of formula IV, (3) subjecting the product to the dehydrative condensation reaction with formalin and the amine of formula Y-H, (4) reacting the obtained compound of formula V with a reducing agent such as sodium borohydride, etc., and (5) dehydrating the resultant compound of formula VI with thionyl chloride and pyridine.
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