| 摘要 |
PURPOSE: To obtain the subject new compound containing a cis-ring connection acting as a strong serotonin retake inhibitor, useful for treating depression, fear spasm, etc. The compound is used as a tablet, etc., and the amount of the compound used is 0.5-50 mg/day. CONSTITUTION: The compound represented by formula(I), wherein R1 to R3 are each H, a halogen, a 1-6C alkyl or the like; R4 is H, a 1-6C alkyl or the like; R5 is an aryl or the like; n is an integer of 1 to 3 such as cis-3a-£(3,4-methylenedioxyphenoxy) methyl|-2,3,3a,7b-tetrahydro-1H-benzo£3,4|cyclobuta£1,2-c|pyrrole, is obtained by reacting a compound of formula (II) with sodium amide to give a compound of formula (III); treating the compound with an inorganic base; reacting the resultant compound with an acetal of N,N-dimethylformamide of the formula (CH3)2NCH(OG)2 to give an ester of formula IV; reducing the ester into an alcohol; and then reacting the alcohol with a compound of the formula R5-OH.
|
