| 摘要 |
<p>1449159 Benzisoindoline derivatives SANDOZ Ltd 28 Sept 1973 [29 Sept 1972 3 Aug 1973] 45477/73 Heading C2C The invention comprises compounds of formula and their acid addition salts, wherein R is H, alkenyl or alkynyl, or alkyl optionally substituted by OH cycloalkyl, Ph (possibly monohalogen, alkyl or alkoxy substituted) or COZ: Z is OH, alkyl, alkoxy, Ph or halophenyl; R 1 , R 2 are each H, halogen or alkyl; and either X=Y=H and rings B and C are in cis-configuration, or X-Y forms an additional bond. In examples, these compounds are prepared by (a) epimerization, (b) N-substitution, (c) reduction or hydrolysis of an N-acyl analogue (A), (d) hydrogenolysis of an N-benzyl compound, (e) reduction of the compound in which X-Y forms a bond, (f) reduction of the 1,3- dioxo analogue (itself derived by dehydrating the tetrahydro - 1,3 - dioxo - 4 - hydroxy - 4- phenylbenzoisoindoline. Compounds (A) may be prepared by cyclizing (e.g.) an appropriate N,N - bis - cinnamyl- or N - cinnamyl - N- phenylpropynyl derivative of CF 3 CONH 2 . Therapeutic compositions, preferably administered orally, comprise compounds of the above formula, which have antidepressant and analgesic activity.</p> |
