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

IF 3.5 3区化学 Q2 CHEMISTRY, APPLIED

Organic Process Research & Development Pub Date : 2024-03-08 DOI:10.1021/acs.oprd.4c00005

Jae-Hong Kweon, Hyungjin Shin, Min Kyoung Lee, Sung Ah Lee, Pargat Singh, Kyeongwon Moon* and In Su Kim*,

引用次数: 0

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 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.

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Tegoprazan 作为钾竞争性酸阻断剂 (P-CAB) 的生产工艺开发

Tegoprazan 是一种选择性钾竞争性酸阻滞剂，2018 年在大韩民国获批用于治疗胃食管反流病（GERD）、侵蚀性食管炎（EE）和非侵蚀性反流病（NERD）。替戈普拉赞含有一个 4,6-二取代的 1H-苯并[d]咪唑核心和一个手性色满醇分子，其复杂性使其成为一种难以商业化制备的分子。我们开发出了一条高效、经济的关键中间体路线，并大大改进了特戈普拉赞的最终制备方法。

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来源期刊

Organic Process Research & Development 化学-应用化学

CiteScore

6.90

自引率

14.70%

发文量

251

审稿时长

2 months

期刊介绍： The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools，process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.