当前位置：
X-MOL 学术
›
Org. Process Res. Dev.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 1: Introduction and Process Overview
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-10-16 , DOI: 10.1021/acs.oprd.0c00248 Hong Ren 1 , Kevin M. Maloney 1 , Kallol Basu 1 , Michael J. Di Maso 1 , Guy R. Humphrey 1 , Feng Peng 1 , Richard Desmond 1 , Douglas A. L. Otte 1 , Embarek Alwedi 1 , Wenjun Liu 1 , Si-Wei Zhang 1 , Siqing Song 1 , Rebecca A. Arvary 1 , Michael A. Zompa 1 , Dan Lehnherr 1 , Gary E. Martin 1 , Hsieh Yao D. Chang 1 , Anne E. Mohan 1 , Francisco J. Guzman 1 , Lisa Jellett 1 , Alfred Y. Lee 1 , Glenn Spencer 1 , Elizabeth S. Fisher 1 , John R. Naber 1 , Hong Gao 1 , Sachin Lohani 1 , Rebecca T. Ruck 1 , Louis-Charles Campeau 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-10-16 , DOI: 10.1021/acs.oprd.0c00248 Hong Ren 1 , Kevin M. Maloney 1 , Kallol Basu 1 , Michael J. Di Maso 1 , Guy R. Humphrey 1 , Feng Peng 1 , Richard Desmond 1 , Douglas A. L. Otte 1 , Embarek Alwedi 1 , Wenjun Liu 1 , Si-Wei Zhang 1 , Siqing Song 1 , Rebecca A. Arvary 1 , Michael A. Zompa 1 , Dan Lehnherr 1 , Gary E. Martin 1 , Hsieh Yao D. Chang 1 , Anne E. Mohan 1 , Francisco J. Guzman 1 , Lisa Jellett 1 , Alfred Y. Lee 1 , Glenn Spencer 1 , Elizabeth S. Fisher 1 , John R. Naber 1 , Hong Gao 1 , Sachin Lohani 1 , Rebecca T. Ruck 1 , Louis-Charles Campeau 1
Affiliation
|
A robust, green, and sustainable manufacturing process has been developed for the synthesis of gefapixant citrate, a P2X3 receptor antagonist that is under investigation for the treatment of refractory and unexplained chronic cough. The newly developed commercial process features low process mass intensity (PMI), short synthetic sequence, high overall yield, minimal environmental impact, and significantly reduced API costs. The key innovations are the implementation of a highly efficient two-step methoxyphenol synthesis, an innovative pyrimidine synthesis in flow, a simplified sulfonamide synthesis, and a novel salt metathesis approach to consistently deliver the correct active pharmaceutical ingredient (API) salt form in high purity.
中文翻译：
柠檬酸Gefapixant（MK-7264）的绿色和可持续制造过程的开发，第1部分：简介和过程概述
已经开发了一种健壮，绿色且可持续的制造工艺来合成柠檬酸吉法匹沙汀，这是一种P2X3受体拮抗剂，目前正在研究中，用于治疗顽固性和无法解释的慢性咳嗽。新开发的商业流程具有低流程质量强度（PMI），合成流程短，总收率高，对环境的影响最小以及API成本大大降低的特点。关键的创新是实施高效的两步甲氧基苯酚合成，流动中的创新嘧啶合成，简化的磺酰胺合成以及新颖的盐复分解方法，以始终如一地提供正确的高纯度活性药物成分（API）盐形式。
更新日期：2020-11-21
中文翻译：
柠檬酸Gefapixant（MK-7264）的绿色和可持续制造过程的开发，第1部分：简介和过程概述
已经开发了一种健壮，绿色且可持续的制造工艺来合成柠檬酸吉法匹沙汀，这是一种P2X3受体拮抗剂，目前正在研究中，用于治疗顽固性和无法解释的慢性咳嗽。新开发的商业流程具有低流程质量强度（PMI），合成流程短，总收率高，对环境的影响最小以及API成本大大降低的特点。关键的创新是实施高效的两步甲氧基苯酚合成，流动中的创新嘧啶合成，简化的磺酰胺合成以及新颖的盐复分解方法，以始终如一地提供正确的高纯度活性药物成分（API）盐形式。
京公网安备 11010802027423号