| 摘要 |
<p>1,174,385. 1 - Pyridyl - 1,2,3,4 - tetrahydroisoquinolines. DR. KARL THOMAE G.m.b.H. 11 March, 1968 [10 March, 1967], No. 11747/68. Addition to 1,173,687. Heading C2C. The invention comprises novel compounds of the general Formula V and acid addition salts thereof, and a process for the preparation of 1 - pyridyl - 1,2,3,4 - tetrahydroisoquinolines corresponding to Formula V and including the 1-(2,3- and 4-pyridyl) derivatives (wherein R 1 and R 2 , which may be the same or different, each represents an alkyl group containing 1 to 3 carbon atoms; and R 3 , R 4 and R 5 , which may be the same or different, each represents a hydrogen atom or a methyl group) and acid addition salts thereof, which process comprises reducing the corresponding 1- pyridyl - 2 - hydroxy - 1,2,3,4 - tetrahydroisoquinoline compound (wherein R 1 to R 5 are as defined above), with hydrogen at above atmospheric pressure in the presence of a hydrogenation catalyst, in the presence of an inert solvent, and if desired converting the compound thereby obtained into an acid addition salt thereof. Compounds of the general Formula II are prepared by a process which comprises cyclisation of a pyridine aldoxime of the Formula III (wherein R 4 is as defined above) with a compound of the Formula IV (wherein R 1 , R 2 , R 3 and R 5 are as defined above; and one of the symbols X and Y represents a hydroxy group, an esterified hydroxy group or a halogen atom and Z and the remaining X or Y symbol each represents a hydrogen atom; or Y together with either X or Z represents a double bond, the remaining X or Z symbol representing a hydrogen atom) in the presence of a strong acid or a Lewis acid. Pharmaceutical compositions having antiphlogistic and antipyretic activity and an activating effect on the enzymes of the liver and containing compounds of the general Formula V defined above, are administered orally, rectally, parenterally or topically in association with a suitable pharmaceutical carrier or excipient.</p> |
