Optimization and process improvement for LCZ696 by employing quality by design (QbD) principles

被引：1
|
作者：
Chen, Zhijun [1 ,4 ]
Wang, Hailong [2 ,4 ]
Wu, Shuming [2 ,4 ]
Wang, Jian [2 ,4 ]
Zhang, Chenxia [2 ,4 ]
Yang, Hua [1 ]
Wang, Zhongqing [2 ,3 ,4 ]
机构：
[1] Cent South Univ, Coll Chem & Chem Engn, Changsha 410083, Peoples R China
[2] Sunshine Lake Pharma Co Ltd, State Key Lab Antiinfect Drug Dev, Dongguan 523871, Peoples R China
[3] Xiangnan Univ, Sch Pharm, Chenzhou 423000, Hunan, Peoples R China
[4] HEC Pharm Grp, HEC Res & Dev Ctr, Dongguan 523871, Peoples R China
来源：
TETRAHEDRON | 2020年 / 76卷 / 46期
基金：
中国国家自然科学基金;
关键词：
LCZ696; DoE; Process; Optimization;
D O I：
10.1016/j.tet.2020.131558
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Efforts toward optimization and improvement for the synthesis of LCZ696 employing design of experiment (DoE) principles are described. By increasing the purity of intermediates and mitigating impurity risk during each step, a telescoped process was developed via removal of isolation of intermediates with the overall yield increased by 28.5% from 45.3% to 73.8%. And the whole production cycle was also shortened from 12 days to 7 days with simplified operations and restored process greenness. Meanwhile, the corresponding impurity profile was thus studied in detail and well documented. (C) 2020 Elsevier Ltd. All rights reserved.
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页数：8
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