Facile and Cost-Effective Route for the Synthesis of Simmerafil
文献类型：期刊论文
| 作者 | Odilov, Abdullajon1,2; Liu, Yin1,2; Hu, Tianwen2,3; Jiang, Xiangrui1,2 ; Suo, Jin1; Tian, Guanghui4; Yang, Feipu1,2; Shen, Jingshan1,2
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| 刊名 | ORGANIC PROCESS RESEARCH & DEVELOPMENT
 |
| 出版日期 | 2021-11-19 |
| 卷号 | 25期号:11页码:2432-2437 |
| 关键词 | simmerafil PDE5 inhibitor salicylamide synthesis |
| ISSN号 | 1083-6160 |
| DOI | 10.1021/acs.oprd.1c00184 |
| 通讯作者 | Yang, Feipu(yangfeipu@simm.ac.cn) |
| 英文摘要 | An improved synthesis of simmerafil, a potent PDE5 inhibitor as a clinical candidate, is described with a 38.1% overall yield and 99.7% purity. Starting from the safe and inexpensive salicylamide (15), the key intermediate 2-propoxybenzimidamide (21), which is also a potential precursor for the preparation of pyrimidinone derivatives, was effectively and conveniently obtained. The subsequent process from 21 to simmerafil was optimized, which makes it more amenable to scale-up. |
| 资助项目 | National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002] ; National Key R&D Program of China[2020YFE0205600] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000726748300006 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/299214]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Yang, Feipu |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Reg, Urumqi, Xinjiang, Peoples R China 4.Vigonvita Life Sci Co Ltd, Suzhou 215123, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Odilov, Abdullajon,Liu, Yin,Hu, Tianwen,et al. Facile and Cost-Effective Route for the Synthesis of Simmerafil[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2021,25(11):2432-2437. |
| APA | Odilov, Abdullajon.,Liu, Yin.,Hu, Tianwen.,Jiang, Xiangrui.,Suo, Jin.,...&Shen, Jingshan.(2021).Facile and Cost-Effective Route for the Synthesis of Simmerafil.ORGANIC PROCESS RESEARCH & DEVELOPMENT,25(11),2432-2437. |
| MLA | Odilov, Abdullajon,et al."Facile and Cost-Effective Route for the Synthesis of Simmerafil".ORGANIC PROCESS RESEARCH & DEVELOPMENT 25.11(2021):2432-2437. |
入库方式： OAI收割
来源：上海药物研究所
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