Synthesis of monoamine oxidase inhibitor intermediate 1，2，3，4-tetrahydro-1-naphthylamine hydrochloride

CHENG Peng; ZENG Qingdong; PENG Yang; ZHANG Wanping; LI Wenjun; LU Zhenhao; YU Yu

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Synthesis of monoamine oxidase inhibitor intermediate 1，2，3，4-tetrahydro-1-naphthylamine hydrochloride

更新时间：2023-12-18

- Synthesis of monoamine oxidase inhibitor intermediate 1，2，3，4-tetrahydro-1-naphthylamine hydrochloride
- Journal of Chongqing Medical University Vol. 36, Issue 6, Pages: 580-582(2013)
- 作者机构：
  
  重庆医科大学药学院药物化学教研室,重庆,400016
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Published：2013，
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CHENG Peng, ZENG Qingdong, PENG Yang, et al. Synthesis of monoamine oxidase inhibitor intermediate 1，2，3，4-tetrahydro-1-naphthylamine hydrochloride. [J]. Journal of Chongqing Medical University 36(6):580-582(2013)
DOI：

CHENG Peng, ZENG Qingdong, PENG Yang, et al. Synthesis of monoamine oxidase inhibitor intermediate 1，2，3，4-tetrahydro-1-naphthylamine hydrochloride. [J]. Journal of Chongqing Medical University 36(6):580-582(2013) DOI：

摘要

目的：设计一种以苯为原料合成单胺氧化酶（monoamine oxidase，MAO）抑制剂中间体1，2，3，4-四氢萘-1-胺盐酸盐的方法。方法：采用Fridel-Crafts酰化反应、Wolf-Kishner-黄明龙还原反应和Harwoth环合反应等方法，以苯为原料，经酰化、还原、环合、缩合、还原以及成盐制得1，2，3，4-四氢萘-1-胺盐酸盐（11）。结果：合成（11）的总收率为43.6%。结论：建立了合成MAO抑制剂中间体1，2，3，4-四氢萘-1-胺盐酸盐的方法，该方法具有原材料廉价易得、反应操作简便以及产品收率较高且品质好等优点，具有一定的工业化生产前景。

Abstract

Objective：To design a method for synthesizing 1，2，3，4-tetrahydro-1-naphthalenamine hydrochloride，which is an impor－tant intermediate for monoamine oxidase（MAO） inhibitors. Methods：1，2，3，4-tetrahydro-1-naphthylamine hydrochloride（11） was synthesized from benzene via acylation，reduction，cyclization，condensation，reduction，and salification by methods of Fridel Crafts acylation，Ｗolf-kishner-HUANG Minglong reduction and Harwoth cyclization. Results：Overall yield for synthesizing 1，2，3，4-te－trahydro-1-naphthylamine hydrochloride（11） was 43.6%. Conclusions：Method for synthesizing 1，2，3，4-tetrahydro-1-naphthale－namine hydrochloride is establish. Optimized synthetic route has advantages in industrial production for its cheap and readily available raw materials，easy in operation，high yield and high quality of products.

关键词

单胺氧化酶抑制剂中间体1，2，3，4-四氢萘-1-胺合成

Keywords

monoamine oxidase inhibitorintermediate1，2，3，4-tetrahydro-1-naphthylamine hydrochloridesynthesize

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