Manufacturing Process Development of Tegoprazan as a Potassium-Competitive Acid Blocker (P-CAB)

被引：5

作者：

Kweon, Jae-Hong ^{[1
,2
]}

Shin, Hyungjin ^{[1
]}

Lee, Min Kyoung ^{[2
]}

Lee, Sung Ah ^{[2
]}

Singh, Pargat ^{[1
]}

Moon, Kyeongwon ^{[1
]}

Kim, In Su ^{[1
]}

机构：

[1] Sungkyunkwan Univ, Sch Pharm, Suwon 16419, South Korea

[2] HK inno N Corp, Proc Dev Ctr, Icheon 17389, South Korea

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2024年 / 28卷 / 04期

基金：

新加坡国家研究基金会;

关键词：

Asymmetric hydrogenation; Manufacturing process; Mitsunobu etherification; Potassium-competitive acid blocker; Tegoprazan; GASTROESOPHAGEAL-REFLUX DISEASE; PUMP INHIBITOR THERAPY; PROTON; DEFINITION; MITSUNOBU; SECRETION; RISK;

D O I：

10.1021/acs.oprd.4c00005

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Tegoprazan, a selective potassium-competitive acid blocker, was approved in 2018 in the Republic of Korea for the treatment of gastroesophageal reflux disease (GERD), erosive esophagitis (EE), and nonerosive reflux disease (NERD). The complexity of tegoprazan, which contains a 4,6-disubstituted 1H-benzo[d]imidazole core and a chiral chromanol moiety, makes it a challenging molecule to prepare on a commercial scale. An efficient and economical route of the key intermediates and a much improved end-game for tegoprazan were developed.

引用

页码：1159 / 1169

页数：11

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