| 摘要 |
1,143,430. 1 - Ethylaminomethyl - 5 - methoxy-benzocyclobutene. CIBA Ltd. 12 Dec., 1966 [28 Dec., 1965], No. 55556/66. Addition to 1,042,197. Heading C2C. 1 - Ethylaminomethyl - 5 - methoxy - benzocyclobutene, a novel compound, and its acidaddition salts, are prepared by (1) reduction of the 1-acetylaminomethyl compound; (2) hydrogenolysis of the corresponding N-aralkylated compounds; or (3) reaction of ethylamine with reactive esters of the appropriate hydroxymethyl compound. 1 - Acetylaminomethyl - 5 - methoxy - benzocyclobutene is prepared by acetylation of the amine. 1 - (N - benzyl - ethylaminomethyl) - 5 - methoxy - benzocyclobutene hydrocFdoride is prepared by reducing 5-metlwxy-benzocyclobutene-1- carboxylic acid (prepared by hydrolysis of the nitrile) to 1 -hydromethyl-5-methoxy-benzocyclobutene, converting this to the p-toluenesulphonate and reacting this with N-ethyl-benzylamine. The compound of the invention, which is stated to have analgesic and anti-tussive properties, and its salts, may be made up into pharmaceutical compositions with suitable carriers. Tablets are described. |
