| 李永,李毅,汤磊,樊玲玲.化学通报,2018,81(1):92-95. |
| HDAC6选择性抑制剂WT161的合成工艺优化 |
| Optimization of Synthetic Process of HDAC6 Selective Inhibitor WT161 |
| 投稿时间：2017-08-06 修订日期：2017-10-26 |
| DOI： |
| 中文关键词: HDAC6抑制剂 WT161合成 工艺优化 |
| 英文关键词:HDAC6 inhibitor WT161 synthesis process optimization |
| 基金项目:贵州省普通高等学校化学药物研发工程中心项目（黔教合KY字[2014]219）；贵州省化学药物开发利用工程实验室（黔发改投资[2015]542号） |
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| 中文摘要: |
| 本文报道了一条新的合成HDAC6选择性抑制剂WT161的路线。以辛二酸单甲酯为起始原料，先后经缩合，取代，还原，脱水共四步反应得到HDAC6选择性抑制剂WT161，总收率64.8 %，目标产物结构均经过1HNMR，13CNMR和 HRMS等确证。优化后的工艺路线原料成本低、反应条件温和、反应后处理更简单、产物收率更高，比较适合较大规模制备。 |
| 英文摘要: |
| A novel synthetic process of [HDAC6 selective inhibitor WT161] has been developed. [HDAC6 selective inhibitor WT161] was synthesized from commercially available monomethyl suberate by four steps, namely condensation, substitution, reduction and dehydration, in 64.8% overall yield. The characterization of the target compound has been carried out by 1H NMR, 13CNMR and HRMS. there are several advantages, such as cost-effectiveness, mild conditions, easy chemical operation and high yield, and easy scale-up production. |
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