| 摘要 |
PURPOSE: A production is provided to obtain cyclic thioamides useful for producing aralkyl and aralkylidene heterocyclic lactams and imides as an agonist and an antagonist of a serotonin 1(5-HT1) receptor helpful for the therapy and prophylaxis of migraine, depression or the like by reacting a specific compound with a dehydrating agent. CONSTITUTION: By reacting a compound of formula I (wherein (b) is 0-3; Y is O, S or the like and: R3 is a halo, cyano or the like), e.g. a compound of formula II with a dehydrating agent (e.g. acetic anhydride), a compound of formula III (e.g. 4-(3,4-dichloro-phenyl)-thiomorpholine-3-one) useful for producing a psychotherapeutic agent is obtained. The reaction product mixture is preferably refluxed under heating for about 1 h. The compound of formula I is obtained by reacting a compound of formula IV (e.g. 3,4-dichloroaniline) with mercaptoacetic acid or the like by reacting the reaction product with a reducing agent (e.g. borane-tetrahydrofuran complex), further reacting with hydrochloric acid and reacting the formed compound with a haloacetic acid (e.g. bromoacetic acid) in the presence of a base.
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