| 郝帅帅,郑璐,陈寅,张桂森,吴庆昆.化学通报,2022,85(2):264-267. |
| GABAA受体激动剂PF0713的合成 |
| Synthesis of GABAA Receptor Agonist PF0713 |
| 投稿时间：2021-06-11 修订日期：2021-06-25 |
| DOI： |
| 中文关键词: 2，6-二((R)-仲丁基)苯酚 麻醉药 工艺优化 合成 Claisen重排反应 手性拆分 |
| 英文关键词:2,6-di((R)-sec-butyl)phenol, Anaesthetic, Process improvement, Synthesis, Claisen rearrangement, Chiral resolution |
| 基金项目:江苏省海洋资源开发研究院开放基金项目(JSIMR202015)资助 |
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| 中文摘要: |
| 2, 6-二((R)-仲丁基)苯酚（PF0713）是在丙泊酚的基础上开发的一种新型烷基酚类静脉麻醉类药物。本文以邻仲丁基苯酚和1-氯-2-丁烯为起始原料，经过一系列反应包括烃化反应，Claisen重排反应和氢化反应以59.2%的收率得到2，6-二仲丁基酚，后经手性拆分得到PF0713，其结构经1H NMR、13C NMR和LC-MS确证。 |
| 英文摘要: |
| 2,6-di((R)-sec-butyl)pheno(PF0713) is a new type of alkylphenol intravenous anesthetic developed on the basis of propofol. In this paper 2-sec-butylphenol and 1-Chlorobut-2-ene were used as raw materials, and 2,6-di-sec-butylphenol was obtained with the yield of 59.2% by a series of reactions including alkylation, Claisen rearrangement and hydrogenation. Then PF0713 was obtained by chiral resolution. The structures were characterized by 1H NMR、13C NMR and LC-MS. |
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