| 摘要 |
3,4-DIHYDRO (AROMATIC[C]) PYRIDINES AND 3,4,5,6-TETRAHYDRO (AROMATIC[C]) PYRAZINES WHICH ARE SUBSTITUTED IN THEIR 1-POSITION BY AN ALKYLTHIO, ALKYLSELENO OR ALKYLTELLURO GROUP, ESPECIALLY 1-ALKYLTHIO-3,4-DIHYDROISOQUINOLINES, ARE PREPARED BY CONTACTING THE CORRESPONDING 2-AROMATIC-ETHYL ISOCYANATE ANALOGUE HAVING AN UNSUBSTITUTED RING CARBON ATOM ADJACENT TO THE RING CARBON ATOM ATTACHED TO THE ETHYL ISOCYANATE ANALOGUE GROUP WITH A COMPOUND INCLUDING THE CORRESPONDING INCIPIENT ALKYL CARBONIUM ION, ESPECIALLY AN ALKYL FLUOROSULPHONIC OR PERFLUORINATED ALKYL SULPHONIC ACID ESTER OR A TRIALKYL-OXONIUM TETRAFLUOROBORATE. The reaction may be carried out in a solvent under reflux conditions at a temperature of 20 DEG to 150 DEG C. The products are intermediates in the preparation of the corresponding 1-amino compounds some of which have been shown to have useful pharmacological activity.
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