| 摘要 |
1,252,320. Dibenzazepine derivatives. SOC. GENERALE DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES. 29 May, 1970 [20 June, 1969], No. 31241/69. Heading C2C. Novel compounds of Formula I in which each of X 1 and X 2 is H, halogen or C 1-4 alkyl and x is 0 or 1 when the -(CH 2 ) x - group is attached to the 3-position of the quinuclidine ring and is 1 or 2 when the -(CH 2 ) x - group is attached to the 2-position of the quinuclidine ring, and their acid addition, and quaternary salts, are prepared by reacting a compound of the Formula II with a compound of Formula III in which Z is a halogen atom or reactive ester radical. 2 - (2 - Chloroethyl) - quinuclidine hydrochloride is prepared from 2-chloromethyl-quinuclidine (itself obtained from the hydrochloride) via the following intermediates 2-cyanomethyl-quinuclidine hydrochloride, 2 - carboxymethylquinuclidine hydrochloride, 2 - ethoxycarhonylmethyl - quinuclidine hydrochloride, 2 - ethoxycarbonylmethyl - quinuclidine and 2 - (2 - hydroxyethyl) -quinuclidine. Pharmaceutical compositions having spasmolytic, antihistaminic, anticholinergic and antidepressant activity comprise one or more of the above novel compounds and a pharmaceutical carrier. The compositions may be administered orally, parenterally or rectally. |
