| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound, capable of manifesting excellent antiemetic actions based on strong antagonistic actions on serotonin S3 and dopamine D2 receptors, having low toxicity and useful as an antiemetic agent. SOLUTION: This (R)-5-bromo-N-(1-ethyl-4-methylhexahydro-1H-1,4-diazepin-6- yl)-2-methoxy-6-methylamino-3-pyridinecarboxamide represented by formula I or its acid addition salt. The compound is obtained by reacting, e.g. a compound represented by formula II with (R)-6-amino-1-ethyl-4-methylhexahydro-1 H-1,4-diazepine represented by formula III. The compound represented by formula II is prepared by starting from, e.g. 2,6-difluoropyridine and the compound represented by formula III is a new substance and is obtained from, e.g. N'- methyl-N-(3-methylbenzyl)ethylenediamine. Furthermore, the reaction is preferably carried out by using 1mol compound represented by formula II and 1-1.5mol compound represented by formula III. |
