二芳基甲基硫醚的合成：一种由1,4-二氮杂二环[2.2.2]辛烷催化的醌甲基化物与有机硫试剂的1,6-共轭加成反应。
Synthesis of diarylmethyl thioethers a DABCO-catalyzed 1,6-conjugate addition reaction of -quinone methides with organosulfur reagents.
作者信息
Shuai Ming-Shan, Guan Xiang, Fei Xing-Hai, Zhang Mao, Fu Xiao-Zhong, He Bin, Zhao Yong-Long
机构信息
State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, and Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University Guiyang 550004 People's Republic of China
出版信息
RSC Adv. 2023 Apr 26;13(19):12982-12990. doi: 10.1039/d3ra01815f. eCollection 2023 Apr 24.
A rapid and simple method was developed for the synthesis of diarylmethyl thioethers a DABCO-catalyzed 1,6-conjugate addition reaction of -quinone methides (-QMs) with organosulfur reagents. A series of diarylmethyl thioethers were synthesized at 13-85% yields by this method. After that, the antibacterial activities of synthesized diarylmethyl thioethers and their derivatives were evaluated. The MIC range (μg mL) against ATCC 25923 and clinically isolated methicillin-resistant was 8-128 and 64-128, respectively.
开发了一种快速简便的方法来合成二芳基甲基硫醚——一种由1,4-苯醌甲基化物（-QMs）与有机硫试剂在1,4-二氮杂双环[2.2.2]辛烷（DABCO）催化下进行的1,6-共轭加成反应。通过该方法以13%-85%的产率合成了一系列二芳基甲基硫醚。之后，对合成的二芳基甲基硫醚及其衍生物的抗菌活性进行了评估。对ATCC 25923和临床分离的耐甲氧西林菌株的最低抑菌浓度范围（μg/mL）分别为8-128和64-128。
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