Advanced Research Institute and Department of Chemistry, Taizhou University, Jiaojiang, Zhejiang 318000, PR China.
Key Laboratory of Green and Precise Synthetic Chemistry, Ministry of Education, Huaibei Normal University, Huaibei, Anhui 235000, PR China.
J Org Chem. 2022 May 20;87(10):6562-6572. doi: 10.1021/acs.joc.2c00136. Epub 2022 Apr 29.
A novel and efficient three-component reaction with two C-N bonds and one C-F bond formation has been reported, which provides a straightforward route to a variety of fluorinated pyrimido[1,2-]indazole derivatives. This transformation has the advantage of excellent functional group compatibility, including aliphatic and aromatic substituents enaminones. Moreover, metal and additives are not necessary for this reaction, which is of great significance for the synthesis and application of fluorinated heterocycles.
本文报道了一种新颖高效的三组分反应，可形成两个 C-N 键和一个 C-F 键，为合成各种氟化嘧啶并[1,2-a]吲唑衍生物提供了一条直接途径。该转化具有优异的官能团相容性的优点，包括脂肪族和芳香族取代基烯胺酮。此外，该反应不需要金属和添加剂，这对于氟代杂环的合成和应用具有重要意义。
