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【结 构 式】 
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【分子编号】12463 【品名】6-Chloro-11H-dibenzo[b,e]azepine 【CA登记号】 |
【 分 子 式 】C14H10ClN 【 分 子 量 】227.69284 【元素组成】C 73.85% H 4.43% Cl 15.57% N 6.15% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(I)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.
| 【1】 Walther, G.; Bechtel, W.D.; Daniel, H.; Brandt, K.; New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine. Arzneim-Forsch Drug Res 1990, 40, 4, 440-6. |
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