Epinastine hydrochloride, WAL-801CL, Elestat, Relestat, Flurinol, Alesion

依匹斯汀Chemical Name: 3-Amino-9,13b-dihydro-1H-dibenz[c,f]imidazol[1,5-a]azepine hydrochloride
CAS No. 80012-43-7 (free base)
项目整合开发状态: Launched-1994
项目研究机构: Boehringer Ingelheim (Originator), Nippon Boehringer Ingelheim (Originator), Allergan (Licensee), Inspire Pharmaceuticals (Comarketer), Sankyo (Comarketer)
合成路线:A new synthesis of epinastine hydrochloride has been described:The reaction of 6-chloro-11H-dibenzo[b,e]azepine (I) with NaCN in DMSO at 90 C gives 11H-dibenzo[b,e]azepine-6-carbonitrile (II),which is reduced with AlH3 (prepared from LiAlH4 and H2SO4 in THF) in THF to afford 6-(aminomethyl)-6,11-dihydro-5H-dibenzo[b,e]azepine (III).Finally,this compound is cyclized with cyanogen bromide in THF and treated with HCl.