First Scale-Up Synthesis of FU-23, a Novel Water-Soluble Pleuromutilin-Derived Antibiotic
文献类型：期刊论文
| 作者 | Fu, Liqiang; Liu, Xin; Cheng, Jianjun; He, Huili; Cai, Zhan; Guo, Xingsheng; Ding, Shi; Yang, Yushe
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| 刊名 | ORGANIC PROCESS RESEARCH & DEVELOPMENT
 |
| 出版日期 | 2010-07 |
| 卷号 | 14期号:4页码:815-819 |
| ISSN号 | 1083-6160 |
| DOI | 10.1021/op100063h |
| 文献子类 | Article |
| 英文摘要 | A first scale-up synthesis of FU-23 (1), a potent and effective water-soluble pleuromutilin-derived antibiotic, is described. The original synthesis from the medicinal chemistry group provided 1 in seven steps and 10.9% overall yield, required four chromatographies and employed expensive reagents such as AgOCN and 4-acetyl-salicoyl chloride. The optimized synthetic route for the preparation of phosphate salt 1 consists of seven linear steps with a 42.8% overall yield. Significant cost reduction and more robust reaction conditions have been developed with no chromatography required at any stage. |
| WOS关键词 | RETAPAMULIN |
| 资助项目 | National Science and Technology Major Project[00000000] ; Key New Drug Creation and Manufacturing Program, China[2009ZX09301-001] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000279874700009 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278865]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Yang, Yushe |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Fu, Liqiang,Liu, Xin,Cheng, Jianjun,et al. First Scale-Up Synthesis of FU-23, a Novel Water-Soluble Pleuromutilin-Derived Antibiotic[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2010,14(4):815-819. |
| APA | Fu, Liqiang.,Liu, Xin.,Cheng, Jianjun.,He, Huili.,Cai, Zhan.,...&Yang, Yushe.(2010).First Scale-Up Synthesis of FU-23, a Novel Water-Soluble Pleuromutilin-Derived Antibiotic.ORGANIC PROCESS RESEARCH & DEVELOPMENT,14(4),815-819. |
| MLA | Fu, Liqiang,et al."First Scale-Up Synthesis of FU-23, a Novel Water-Soluble Pleuromutilin-Derived Antibiotic".ORGANIC PROCESS RESEARCH & DEVELOPMENT 14.4(2010):815-819. |
入库方式： OAI收割
来源：上海药物研究所
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