摘要
目的合成选择性去甲肾上腺素再摄取抑制剂类抗抑郁药物盐酸维洛沙嗪。方法以2-乙氧基苯酚为原料,经环氧化、胺解、成盐反应得到维洛沙嗪盐酸盐。结果与结论经过3步反应合成目标化合物维洛沙嗪,总收率为28.4%。此外,还分离纯化得到两个盐酸维洛沙嗪的有关物质。目标化合物的结构均经1H-NMR和MS谱确证。
Viloxazine is a bicyclic antidepressant morpholine derivative. It acts as a selective norepinephrine reuptake inhibitor（NRI）. Besides, viloxazine has two stereoisomers, the （S）- （ - ）-isomer being five times as pharmacologically active as the（R）-（ ＋ ）-isomer. Its hydrochloride was approved in Italy,England,Germany for the treatment of ADHD （ attention deficit hyperactivity disorder） and depressive disorder. Based on the synthetic method of viloxazine hydrochloride reported in a patent, its preparation process were optimized. The synthesis of viloxazine hydrochloride（ 1 ） has been accomplished from 2-ethoxyphenol as starting materi- al, through three steps in 28.4% overall yield. Besides, two related compounds （5 and 6） were isolated from the reaction. Their structures were confirmed by 1H-NMR and ESI-MS.
出处
《中国药物化学杂志》
CAS
CSCD
2015年第6期450-452,共3页
Chinese Journal of Medicinal Chemistry
关键词
抗抑郁
合成
维洛沙嗪
有关物质
antidepressant
synthesis
viloxazine
related compound
