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

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-b...

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Bibliographic Details
Published in:Organic process research & development 2024-04, Vol.28 (4), p.1159-1169
Main Authors: Kweon, Jae-Hong, Shin, Hyungjin, Lee, Min Kyoung, Lee, Sung Ah, Singh, Pargat, Moon, Kyeongwon, Kim, In Su
Format: Article
Language:English
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Summary: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.
ISSN:1083-6160
1520-586X
DOI:10.1021/acs.oprd.4c00005