| 摘要 |
<p>1,140,387. Tetrahydro - thiazolo - [5,4c]- pyridines. DR. KARL THOMAE, G.m.b.H. 15 July, 1966 [23 July, 1965], No. 31938/66. Heading C2C. [Also in Division A5] Novel compounds of the formula (wherein R 1 is H, C 1-6 alkyl, C 2-6 alkenyl, halo C 2-6 alkenyl, C 3-8 cycloalkyl, C 6-10 aryl, C 7-9 aralkyl, aromatic or aliphatic carboxylic or sulphonic acyl, carbamoyl or amidino; R 2 is H, C 1-6 alkyl, C 2-6 alkenyl, halo C 2-6 alkenyl, or cycloalkyl, or NR 1 R 2 is a heterocyclic ring which may contain a further hetero atom and/or be OH, methyl or phenyl substituted; R 3 is H, C 1-6 alkyl, C 2-6 alkenyl, halo C 2-6 alkenyl, C 3-8 cycloalkyl, C 6-10 aryl, C 7-9 aralkyl, aromatic or aliphatic carboxylic or sulphonic acyl, carbamoyl, thiocarbamoyl or amidino; and where alkyl groups R 1 , R 2 and/or R 3 may be OH, alkoxy, aryloxy, cycloalkyl, carboxy, carbalkoxy or amido substituted, and aromatic groups R 1 , R 2 and/or R 3 may be halogen, OH, alkyl, alkoxy, alkylthio, alkylsulphonyl, alkylenedioxy, amino, alkylamino, acylamino or aminosulphonyl substituted. R 4 and R 5 are H, alkyl, aryl or aralkyl; and R is a bond or a C 1-3 hydrocarbon chain) and acid-addition salts thereof, are prepared from hydrohalic acid salts of the appropriate 3-bromo-4-piperidones and thioureas or thioamides. Products wherein R 3 is aryl may be hydrolysed, provided R 1 is not aryl, to the corresponding compounds wherein R 3 is H, which compounds may in turn be reacted with appropriate reagents to replace the H atom R 3 by another radical or group R 3 (except aryl).</p> |
