Optimization of synthetic technological conditions for 1-aminomethyl-1，2，3，4-tetrahydroisoquinoline hydrochloride with orthogonal design

ZHANG Xinyu; CHENG Xunguan; ZHENG Xiaohong; WANG Yu; PENG Yang; YU Yu

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Optimization of synthetic technological conditions for 1-aminomethyl-1，2，3，4-tetrahydroisoquinoline hydrochloride with orthogonal design

更新时间：2023-12-18

- Optimization of synthetic technological conditions for 1-aminomethyl-1，2，3，4-tetrahydroisoquinoline hydrochloride with orthogonal design
- Journal of Chongqing Medical University Vol. 37, Issue 3, Pages: 224-228(2012)
- 作者机构：
  
  重庆医科大学药学院药物化学与生物材料研究室、重庆高校药物工程研究中心,重庆,400016
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Published：2012，
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ZHANG Xinyu, CHENG Xunguan, ZHENG Xiaohong, et al. Optimization of synthetic technological conditions for 1-aminomethyl-1，2，3，4-tetrahydroisoquinoline hydrochloride with orthogonal design. [J]. Journal of Chongqing Medical University 37(3):224-228(2012)
DOI：

ZHANG Xinyu, CHENG Xunguan, ZHENG Xiaohong, et al. Optimization of synthetic technological conditions for 1-aminomethyl-1，2，3，4-tetrahydroisoquinoline hydrochloride with orthogonal design. [J]. Journal of Chongqing Medical University 37(3):224-228(2012) DOI：

摘要

目的：利用正交实验法优选药物重要中间体1-氨甲基-1，2，3，4-四氢异喹啉盐酸盐（1）的合成工艺条件。方法：采用正交实验方法，考察合成（1）中的酰化、邻苯二甲酰亚胺N-烃化、Bischler-Napieralski反应、肼解与还原等主要反应的关键条件对收率的影响，筛选出主要反应的优选实验条件。结果：合成（1）的总收率达到了62.4%，约为原来总收率的2.5倍。结论：该合成工艺路线具有原料廉价易得、反应操作简便、兼顾环保以及产品收率高且品质好等优点；具有较好的工业化生产前景。

Abstract

Objective：To optimize the synthetic technological conditions of 1-aminomethyl-1，2，3，4-tetrahydroisoquinoline hy－drochloride as important intermediate for drugs by orthogonal experimental method. Methods：The target product was synthesized from β-phenethylamine by phthalimide N-hydrocarbylation reaction，Bischler-Napieralski reaction，cyclization with Bischler-Napieralski method，hydrazinolysis reaction，reduction and salification. The key factors on each reaction were discussed separately and optimized by orthogonal experiment. Results：The overall yield was 65%，2.5 times as much as that of the reported. Conclusion: The optimized synthetic route has promise in industrial production for its cheap and readily available raw materials，easy and environmentally-friend processes，high yield and good quality of products.

关键词

1-氨甲基-1，2，3，4-四氢异喹啉合成正交实验工艺条件中间体

Keywords

1-aminomethyl-1，2，3，4-tetrahydroisoquinolinesynthesisorthogonal experimenttechnological conditionintermediate

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