Zhang Guo-Fu, Han Lin-Jun, Guan Chen-Fei, Ding Cheng-Rong
College of Chemical Engineering, Zhejiang University of Technology, 18 Chaowang Road, Hangzhou 310014, P. R. China.
J Org Chem. 2023 Sep 15;88(18):13142-13148. doi: 10.1021/acs.joc.3c01364. Epub 2023 Aug 31.
With the increasing relevance of organophosphorus fluorine compounds in the pharmaceutical industry, their synthesis has attracted great attention. Herein, we report an efficient fluorination strategy for P(O)-H and P(O)-OH compounds using sulfuryl fluoride as the fluorination reagent. Avoiding the use of expensive or complex prepreparation reagents for fluoridation, this strategy could conveniently construct a variety of fluorophosphonates and phosphonofluoridates under mild conditions and without additional oxidants.
随着有机磷氟化合物在制药工业中的相关性日益增加,它们的合成引起了极大关注。在此,我们报道了一种使用硫酰氟作为氟化试剂对P(O)-H和P(O)-OH化合物进行有效氟化的策略。该策略避免使用昂贵或复杂的预制备氟化试剂,能够在温和条件下且无需额外氧化剂的情况下方便地构建各种氟代膦酸酯和膦酰氟化物。