| 摘要 |
Novel 1,4 - bis - (acetyl) - piperazines of Formula I <FORM:1058623/C2/1> wherein each X represents a phenyl group which may be substituted by one or more hydroxy, alkyl, alkoxy, alkoxycarbonyl or carbamoyl groups, the alkyl and alkoxy groups containing from 1-6 carbon atoms, are prepared by reacting a 1,4-bis-(haloacetyl)-piperazine with an alkali metal phenolate, or by reacting piperazine or an acid addition salt thereof with a phenylglycollic halide, anhydride or ester, and additionally, when X is a hydroxyphenyl group by reacting the corresponding benzyloxyphenyl compound with hydrogen in the presence of a catalyst. The alkali metal phenolate used in the first reaction above may be previously prepared by reacting phenol wth an alkali metal. 1,4 - Bis - [(2 - benzyloxyphenoxy) - acetyl]-piperazine is prepared by reacting o-monobenzylcatechol with 1,4-bis-(chloroacetyl)-piperazine in the presence of sodium. Therapeutic compositions having central nervous systemdepressant, analgesic and antitussive activity, and which may be administered orally, parenterally or rectally, contain as active ingredient a compound of Formula I above. |
