Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Central South University , Changsha 410083, China.
Org Lett. 2017 Mar 17;19(6):1410-1413. doi: 10.1021/acs.orglett.7b00335. Epub 2017 Mar 3.
A transition-metal-free decarboxylative fluorination of electron-rich five-membered heteroaromatics, including furan-, pyrazole-, isoxazole-, thiophene-, indole-, benzofuran- and indazolecarboxylic acids, with Selectfluor is reported. Fluorinated dimer products were observed for nitrogen-containing heteroaromatic carboxylic acids, such as indole and pyrazole. An effective method has been developed to synthesize the monomer of 2- and 3-fluoroindoles with LiCO as base at low temperature.
本文报道了一种无过渡金属参与的富电子五元杂芳香族羧酸（如呋喃、吡唑、异噁唑、噻吩、吲哚、苯并呋喃和吲唑羧酸）的脱羧氟化反应，所用试剂为 Selectfluor。含氮杂芳香羧酸如吲哚和吡唑会生成氟化二聚产物。本文还发展了一种以 LiCO3 为碱、在低温下合成 2-和 3-氟吲哚单体的有效方法。
