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Direct Synthesis of Monofluoromethylthioesters from Acyl Chlorides with Elemental Sulfur and Fluoroiodomethane
European Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2024-04-24 , DOI: 10.1002/ejoc.202400296
Chen-Chen Hu 1 , Yu-Yang Zhang 2 , Zeguo Fang 2 , Feng-Ling Qing 3
Affiliation  

We report an unprecedented Ni‐catalyzed direct monofluoromethylthiolation of acyl chlorides, in situ generated from carboxylic acids, with elemental sulfur (S8) as the S source and fluoroiodomethane (ICH2F) as the CH2F radical source to produce a series of monofluoromethylthioesters in moderate to good yields. This approach features excellent functional group tolerance and broad substrate scope. Additionally, the late‐stage monofluoromethylthiolation of complex bioactive molecules can also be accomplished using this method.

中文翻译:

酰氯与单质硫和氟碘甲烷直接合成单氟甲基硫酯

我们报道了一种前所未有的镍催化酰氯直接单氟甲硫基化反应,由羧酸原位生成,以元素硫(S8)作为S源,氟碘甲烷(ICH2F)作为CH2F自由基源,以中等至良好的速度生产一系列单氟甲硫酯。产量。该方法具有优异的官能团耐受性和广泛的底物范围。此外,复杂生物活性分子的后期单氟甲硫基化也可以使用这种方法完成。
更新日期:2024-04-24
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