| 摘要 |
<p>1,054,092. Bicyclo [2.2.2]-octanes. E. I. DU PONT DE NEMOURS & CO. April 23, 1964 [May 1, 1963], No. 16927/64. Heading C2C. [Also in Division C5] New compounds are of general formula where R is hydrogen or alkyl (1-6 C); R 1 is -N=CH-Ph, polymethyleneimine (4-6 C), or -NR 2 R 3 , R 2 being hydrogen or alkyl (1-6 C) optionally substituted by hydroxy, alkoxy (1-2 C), NH 2 , NHalkyl or N(alkyl) 2 (said alkyl having 1-4 C), and R 3 having one of the meanings of R 2 or being Cl, Br, CHO, CH 2 COOH, CH 2 COOCH 3 or CH 2 COOC 2 H 5 ; and salts of the basic compounds; and N-oxides of compounds where R 1 is dialkylamino or polymethyleneimino. Various methods of preparation are described. The 1-aminobicyclooctane is prepared by ammoniation of the 1,4-diiodo compound, and with the 4-alkyl compounds is also prepared from corresponding bicyclooctane carboxylic acids by the Schmidt technique. The other compounds are all obtained from these with appropriate reagents; or from bicyclooctanes having in the 1-position an N-acetyl or cyclic lactam group by hydrolysis or reduction; or by replacing a 1-bromo atom by formamido. Starting materials obtained in examples are: 1,2,3,4 - tetrachlorobicyclooct - 2 - ene, 1,4- dichlorobicyclooctane and the 1,4-dihydroxy and 1,4-diiodo compounds; 1-methyl-4-carboxy - bicyclooctane; 1 - methyl - bicyclooctan- 4-ol-2-one (and its hydrazone) and 1-methyl-4 hydroxy- and -acetamido-bicyclooctane; 1-(N- methyl, N-acetyl, N-butyryl and N-3-methoxypropionyl - aminobicyclooctanes ; N-bicyclooctyl-pyrrolidin-2-one. Pharmaceutical compositions (e.g. tablets, capsules, solutions) comprise the new antiviral compounds with carriers, and they may also be incorporated into animal feeds and concentrates therefor.</p> |
