Key Laboratory of Science and Technology of Eco-Textiles, Ministry of Education, College of Chemistry, Chemical Engineering and Biotechnology , Donghua University , 2999 North Renmin Lu , Shanghai 201620 , China.
Key Laboratory of Organofluorine Chemistry, Center for Excellence in Molecular Synthesis , Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 345 Lingling Lu , Shanghai 200032 , China.
Org Lett. 2018 Sep 7;20(17):5497-5501. doi: 10.1021/acs.orglett.8b02451. Epub 2018 Aug 27.
The direct synthesis of C(CF)Me-substituted heteroarenes by decarboxylative 1,1-dimethyltrifluoroethylation of heteroarenes with 3,3,3-trifluoro-2,2-dimethylpropanoic acid is reported. This method does not need the transition-metal catalyst, and the base is crucial for this reaction. A series of previously unknown C(CF)Me-containing heteroarenes were obtained in high yields and have potential applications in the drug discovery process.
本文报道了通过 3,3,3-三氟-2,2-二甲基丙酸对杂芳烃进行脱羧 1,1-二甲基三氟乙基化反应，直接合成 C(CF)Me 取代的杂芳烃。该方法不需要过渡金属催化剂，而碱对该反应至关重要。一系列以前未知的含 C(CF)Me 的杂芳烃以高产率得到，并有可能在药物发现过程中得到应用。
