通过唑类与溴二氟乙酸酯和单质硫反应，亚硫酸盐促进合成N-二氟甲基硫脲
Sulfite-Promoted Synthesis of N-Difluoromethylthioureas via the Reaction of Azoles with Bromodifluoroacetate and Elemental Sulfur.
作者信息
Deng Jian-Chao, Gao Yong-Chao, Zhu Zhu, Xu Li, Li Zhao-Dong, Tang Ri-Yuan
机构信息
Department of Applied Chemistry, College of Materials and Energy , South China Agricultural University , Guangzhou 510642 , China.
Key Laboratory of Natural Pesticide & Chemical Biology, Ministry of Education , South China Agricultural University , Guangzhou 510642 , China.
出版信息
Org Lett. 2019 Jan 18;21(2):545-548. doi: 10.1021/acs.orglett.8b03876. Epub 2018 Dec 31.
A sulfite-promoted transformation of azoles into N-difluoromethylthioureas through N-difluoromethylation and sulfuration has been developed. In this reaction, inexpensive ethyl bromodifluoroacetate and nontoxic elemental sulfur were used as the difluoromethylation and sulfuration reagents, respectively. A variety of azoles, including benzimidazoles, imidazoles, and triazoles, performed well to afford a broad range of azole thioureas in moderate to good yields.
通过N-二氟甲基化和硫化反应，已开发出一种亚硫酸盐促进的唑类化合物转化为N-二氟甲基硫脲的方法。在该反应中，分别使用廉价的溴二氟乙酸乙酯和无毒的单质硫作为二氟甲基化试剂和硫化试剂。包括苯并咪唑、咪唑和三唑在内的多种唑类化合物表现良好，能以中等至良好的产率得到一系列唑类硫脲。
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