| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for producing epinastine via a new intermediate which is safely synthesizable at a low cost.SOLUTION: Epinastine is produced by reacting 5H-dibenz[b, e]azepine-6,11-dihydro-6-methanamine with an N-(iminoalkoxymethyl)carbamic acid ester to synthesize an N-(9,13-dihydro-1H-dibenz[c, f]imidazo[1,5-a]azepin-3-yl)-carbamic acid ester as an intermediate and treating the intermediate with an acid (process A). As an alternative, epinastine is produced by reacting an acid salt of 5H-dibenz[b, e]azepine-6,11-dihydro-6-methanamine with an N-(iminoalkoxymethyl)carbamic acid ester to synthesize an {imino[N-(5H-dibenz[b, e]azepin-6-yl)methylamino]methyl}carbamic acid ester as an intermediate and treating the intermediate with an acid (process B). |
