Manufacturing Process Development of Tegoprazan as a Potassium-Competitive Acid Blocker (P-CAB)
Jae‐Hong Kweon, Hyungjin Shin, Min Kyoung Lee, Sung Ah Lee, Pargat Singh, Kyeongwon Moon, In Su Kim
Abstract
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 1 H -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.
Topics & Concepts
Process developmentPotassiumProcess (computing)Manufacturing processChemistryCombinatorial chemistryBusinessComputer scienceProcess managementOrganic chemistryMaterials scienceComposite materialOperating systemDrug Solubulity and Delivery SystemsCrystallization and Solubility StudiesGastroesophageal reflux and treatments