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研究论文

碱促进下空气氧化制备α-芳甲酰基硫代酰胺的便捷方法

王聪a,b, 姚瑶瑶a, 谢珺a, 王建塔a, 王飞清c, 张吉泉a, 汤磊a,b,d   

  1. a 贵州医科大学药学院 贵州贵阳 550025;
    b 贵州医科大学 药用植物功效与利用国家重点实验室 贵州贵阳 550014;
    c 贵州中医药大学第一附属医院 贵州贵阳 550001;
    d 贵州省化学合成药物研发利用工程技术研究中心 贵州贵阳 550004
  • 收稿日期:2020-06-04 修回日期:2020-07-30 出版日期:2030-01-01 发布日期:2020-08-19
  • 通讯作者: 汤磊 E-mail:kingland1@163.com,tlei1974@hotmail.com
  • 基金资助:
    国家自然科学基金(No.81560559,81703356)、贵州省高等学校药物化学工程研究中心(No.黔教合KY字[2014]219)、贵州省科技厅社发公关项目(No.黔科合SY[2015]3030)资助项目、贵州省卫健委科学技术基金gzwjk2019-1-179、贵州医科大学博士后流动站.

Convenient Method for Preparing α-ketoarylthioamide by Air Oxidation under Base Conditions

Wang Conga,b, Yao Yaoyaoa, Xie Juna, Wang Jiantaa, Wang Feiqingc, Zhang Jiquana, Tang Leia,b,d   

  1. a College of Pharmacy, Guizhou Medical University, Guiyang, 550025;
    b State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang, 550014;
    c The First Affiliated Hospital of Guizhou University of Traditional Chinese Medicine, Guiyang, 550001;
    d Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang, 550004
  • Received:2020-06-04 Revised:2020-07-30 Online:2030-01-01 Published:2020-08-19
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 81560559, 81703356), Guizhou High-School Engineering Research Center for Medicinal Chemistry (NO. QJHKY[2014]219), the Scientific and Technological Foundation of Guizhou Health Committee gzwjk2019-1-179, and Mobile Postdoctoral Center of Guizhou MedicalUniversity.

报道了一种实用的空气氧化制备α-芳甲酰基硫代酰胺的方法.在空气氛围下,以K2CO3为碱,二甲基亚砜为溶剂,120 ℃条件下,α-苄基硫代酰胺经氧化以42%~85%的产率得到α-芳甲酰基硫代酰胺.该反应无需金属参与,具有良好的底物适用性和原子经济性,为α-芳甲酰基硫代酰胺的合成提供了一种高效,经济,绿色,简便的方法.

关键词: 空气, DMSO-K2CO3, 绿色氧化, α-芳甲酰基硫代酰胺

A practical method for preparing α-ketoaryl thioamide by air oxidation has been developed. Under air atmosphere, and in the presence of K2CO3 in DMSO as solvent at 120 ℃, a variety of α-ketoaryl thioamides were obtained from aryl thioamide in the yield of 42%~85%. This reaction has good substrate applicability, metal-free and atomic economy, and provides an efficient, economical, green and convenient method for the synthesis of α-ketoaryl thioamide.

Key words: air, DMSO-K2CO3, green oxidation, α-ketoaryl thioamide