School of Chemistry and Materials Science, Heilongjiang University, Harbin 150080, P. R. China.
Org Biomol Chem. 2023 Feb 22;21(8):1814-1820. doi: 10.1039/d3ob00096f.
A protocol for metal and oxidant free photoredox catalyzed trifluoromethylation of 2-indazoles was developed by using Eosin Y as the photocatalyst and recoverable ionic liquids as the solvents. A series of trifluoromethylated products were obtained in moderate to good yields in this protocol under mild conditions. The reaction proceeded a free-radical mechanism with a broad substrate range, excellent regioselectivity, and good functional group tolerance. Furthermore, the utility of this protocol was demonstrated by the synthesis of a highly selective ligand for estrogen receptor beta (ERβ) and the drug granisetron. The protocol provides a mild and environmentally friendly solution for trifluoromethylation reaction.
开发了一种以曙红 Y 为光催化剂、可回收离子液体为溶剂的无金属和氧化剂的光氧化还原催化 2-吲哚三氟甲基化反应的方案。在温和的条件下，该方案可以以中等至良好的收率得到一系列三氟甲基化产物。该反应通过自由基机制进行，具有广泛的底物范围、优异的区域选择性和良好的官能团耐受性。此外，该方案的实用性通过合成雌激素受体β（ERβ）的高选择性配体和药物格拉司琼得到了证明。该方案为三氟甲基化反应提供了一种温和环保的解决方案。
