| 摘要 |
1313963 Quinolyl/quinuclidyl ketones and carbinols; substituted-quinolyl lithium compounds F HOFFMANN-LA ROCHE & CO AG 19 April 1971 [16 March 1970] 24189/71 Headings C2C and C2J The title ketones (VI) and carbinols (I, II): wherein m is 1-or 2, R 1 is H, halogen, OH, CF 3 or C 1-7 alkyl or alkoxy,-or (R 1 ) m is methylenedioxy, and R 2 is vinyl or Et, and their enantiomers, racemates and acid addition salts, are prepared by reacting together the corresponding quinolyl-Li (III) with either an epimeric 2-formyl-5- R 2 -quinuclidine (giving I, II) or an epimeric ester of a 5-R 2 -quinuclidine-2-carboxylic acid (giving VI), and in the latter case optionally reducing VI to give I, II. Compounds III, prepared in examples by reacting a corresponding 4-bromoquinoline (from the 4-hydroxyquinoline with PBr 3 + PoBr 3 ) with LiBu, are (except when R 1 =H) claimed per se. Also described are the optical resolution of XCH 2 CHOHCCl 3 (X=3- ethyl - 4 - pyridyl) and the preparation of YCH 2 CHOHCHCl 2 (Y=3-ethyl- or 3-vinyl-4- piperidyl). Therapeutic compositions for oral, parenteral or rectal administration comprise the above carbinols (I, II), which have antimalarial and antiarrhythmic properties. |
