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Citation: Yin Yihu, Xue Yutao, Dou Chunshui, Yao Qingqiang. Process Optimization for Synthesis of Antihypertensive Agent Macitentan[J]. Chemistry, ;2018, 81(4): 380-383. shu

Process Optimization for Synthesis of Antihypertensive Agent Macitentan

School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences; Institute of Materia Medical, Shandong Academy of Medical Sciences; Key Laboratory for Biotech-Drugs Ministry of Health; Key Laboratory for Rare & Uncommon Diseases of Shandong Province, Jinan 250062

Corresponding author: Yao Qingqiang, yao_imm@163.com
Received Date: 3 January 2018
Accepted Date: 30 January 2018

Figures(1)

Using methyl 4-bromophenylacetate as the starting material, Macitentan was synthesized by a 6-step reaction of nucleophilic substitution of carbon anion, ring-closing reaction, chlorination, nucleophilic substitution of nitrogen anion, nucleophilic substitution of oxygen anion, and the synthetic process was also optimized. The structures of the intermediates and products were confirmed by ¹H-NMR and ESI-MS. The optimized process improves the purity of the intermediate, the operation is more simple and more conducive to industrial production.
- Macitentan,
- Synthesis,
- Hypertension
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