Improved Practical Synthesis of DY-038, an Oral Available Antiplatelet Agent
文献类型：期刊论文
| 作者 | Cao, Yangzhi1,2; Kong, Deyu1; Sun, Lulu1; Meng, Xin1; Zhang, Yinyong1; Guo, Bin1 ; Yang, Yushe1,2
|
| 刊名 | CHEMISTRYSELECT
 |
| 出版日期 | 2021-04-08 |
| 卷号 | 6期号:13页码:3183-3186 |
| 关键词 | antiplatelet agent cyclization DY-038 process development sulfonamides |
| ISSN号 | 2365-6549 |
| DOI | 10.1002/slct.202100599 |
| 通讯作者 | Yang, Yushe(ysyang@simm.ac.cn) |
| 英文摘要 | Recently, we reported the promising activity of a series of novel bicyclic pyridine derivatives as antiplatelet agents. Herein, we describe a modified and improved chemical synthesis of the lead compound, 1-(3-cyano-5-oxo-5,7-dihydrofuro[3,4-b]pyridin-2-yl)-4-methyl-N-((4-methylbenzyl)sulfonyl)piperidine-4-carboxamide (1), with the aim to produce from milligrams to 10 g of the pure compound that is necessary for the preclinical studies. This novel process is one step shorter and starts from cheap materials, achieving a sevenfold of the total yield from 0.7 % to 5 %. Additionally, it also avoids the use of palladium on carbon as well as all of the steps involve simple purifications without chromatography. |
| WOS关键词 | MYOCARDIAL-INFARCTION ; GUIDELINES ; MANAGEMENT ; THERAPIES ; RECEPTOR |
| 资助项目 | National Natural Science Foundation of China[21332003] ; Youth Innovation Promotion Association of Chinese Academy of Sciences[2016262] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000656857900016 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/297024]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Yang, Yushe |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Sch Pharm, 19 A Yuquan Rd, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Cao, Yangzhi,Kong, Deyu,Sun, Lulu,et al. Improved Practical Synthesis of DY-038, an Oral Available Antiplatelet Agent[J]. CHEMISTRYSELECT,2021,6(13):3183-3186. |
| APA | Cao, Yangzhi.,Kong, Deyu.,Sun, Lulu.,Meng, Xin.,Zhang, Yinyong.,...&Yang, Yushe.(2021).Improved Practical Synthesis of DY-038, an Oral Available Antiplatelet Agent.CHEMISTRYSELECT,6(13),3183-3186. |
| MLA | Cao, Yangzhi,et al."Improved Practical Synthesis of DY-038, an Oral Available Antiplatelet Agent".CHEMISTRYSELECT 6.13(2021):3183-3186. |
入库方式： OAI收割
来源：上海药物研究所
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