| 摘要 |
The invention comprises: (a) the preparation of iminostilbene (5-dibenzo[b.f]azepine) derivatives of the general formula <FORM:0921961/IV(a)/1> (wherein the two symbols X represent hydrogen or chlorine atoms or identical C1-4 alkyl radicals, Alkylene represents a C2-6 alkylene radical, and R represents a C1-4 hydroxyalkyl radical) by reacting a reactive ester of a compound of the general formula <FORM:0921961/IV(a)/2> with an N-substituted piperazine of the general formula <FORM:0921961/IV(a)/3> (b) the preparation of compounds of the general formula I above wherein R represents a C2-8 alkanoyloxyalkyl radical by esterifying the compounds wherein R represents a C1-4 hydroxyalkyl radical; (c) 5-[31-(411-hydroxyethylpiperazino) -propyl]-iminostilbene and its 3,7-dichloro and 3,7-dimethyl derivatives, 5-[21-(411 - g - hydroxypropylpiperazino)-ethyl]-2,8-dichloroiminostiblene, and 5-[31-(411-acetoxyethylpiperazino) - propyl] - 3,7-dichloroiminostilbene. The products of processes (a) and (b) have sedative, anticonvulsive, antiallergic, antiemetic, antiphlogistic and antipyretic activity. They form mono- and di-addition salts with inorganic and organic acids. Reactive esters of compounds II are prepared by reacting iminostilbene or chloro or alkyl derivatives thereof with reactive diesters of alkanediols, preferably those having two different acid components (e.g. a -bromo-b - or -o -chloroalkanes, or arylsulphonic esters of chloro- or bromo-alkanols). |
