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Optimization and Development of a Scalable Palladium-Catalyzed C-H Activation Process for the Geometry-Selective Preparation of Kilograms of YLF466D, a Potent AMP-Activated Protein Kinase Activator

文献类型：期刊论文

作者Yin, Jianpeng1; Zhan, Desheng1; Ma, Hui2; Liu, Huanan2; Yu, Lifang2; Zhang, Yangming1,2; Nan, Fajun1,2,3
刊名ORGANIC PROCESS RESEARCH & DEVELOPMENT
出版日期2021-10-15
卷号25期号:10页码:2260-2269
关键词YLF466D AMPK activator glucose metabolism lipid metabolism MIRI domino reaction C-H activation
ISSN号1083-6160
DOI10.1021/acs.oprd.1c00150
通讯作者Zhang, Yangming(ymzhang@simm.ac.cn) ; Nan, Fajun(fjnan@simm.ac.cn)
英文摘要Adenosine 5'-monophosphate-activated protein kinase (AMPK) activator YLF466D is a promising preclinical drug candidate to treat metabolic diseases and myocardial ischemia-reperfusion injury (MIRI). Herein, we report our efforts on optimization and development of a practical and scalable process for the preparation of YLF466D in kilogram scale. The process features a palladium-catalyzed C-H activation under mild reaction conditions, geometry selectivity, effective impurities purging, and low levels of residual solvents in the final active pharmaceutical ingredient (API). We applied this process successfully to prepare more than 17 kg (3.0-3.6 kg per batch) of YLF466D to support its preclinical study.
WOS关键词ISCHEMIA
资助项目National Science and Technology Major Project[2018ZX09711002-012-005]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000709699500009
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/298759]  
专题新药研究国家重点实验室
通讯作者Zhang, Yangming; Nan, Fajun
作者单位1.Yantai Inst Mat Med, Yantai Key Lab Nanomed & Adv Preparat, Yantai 264000, Shandong, Peoples R China
2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Yin, Jianpeng,Zhan, Desheng,Ma, Hui,et al. Optimization and Development of a Scalable Palladium-Catalyzed C-H Activation Process for the Geometry-Selective Preparation of Kilograms of YLF466D, a Potent AMP-Activated Protein Kinase Activator[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2021,25(10):2260-2269.
APA Yin, Jianpeng.,Zhan, Desheng.,Ma, Hui.,Liu, Huanan.,Yu, Lifang.,...&Nan, Fajun.(2021).Optimization and Development of a Scalable Palladium-Catalyzed C-H Activation Process for the Geometry-Selective Preparation of Kilograms of YLF466D, a Potent AMP-Activated Protein Kinase Activator.ORGANIC PROCESS RESEARCH & DEVELOPMENT,25(10),2260-2269.
MLA Yin, Jianpeng,et al."Optimization and Development of a Scalable Palladium-Catalyzed C-H Activation Process for the Geometry-Selective Preparation of Kilograms of YLF466D, a Potent AMP-Activated Protein Kinase Activator".ORGANIC PROCESS RESEARCH & DEVELOPMENT 25.10(2021):2260-2269.

入库方式： OAI收割

来源：上海药物研究所

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