Department of Applied Chemistry, Waseda University, 513 Wasedatsurumakicho, Shinjuku, Tokyo 162-0041, Japan.
Org Lett. 2022 May 6;24(17):3270-3274. doi: 10.1021/acs.orglett.2c01149. Epub 2022 Apr 26.
A ring-opening fluorination of isoxazoles has been developed. Upon treatment of isoxazoles with an electrophilic fluorinating agent (Selectfluor), fluorination followed by deprotonation leads to tertiary fluorinated carbonyl compounds. This method features mild reaction conditions, good functional group tolerance, and a simple experimental procedure. Diverse transformations of the resulting α-fluorocyanoketones were also demonstrated, furnishing a variety of fluorinated compounds.
发展了一种异恶唑的开环氟化反应。异恶唑与亲电氟化试剂（Selectfluor）反应，首先发生氟化反应，然后再脱质子化，得到叔氟代羰基化合物。该方法具有反应条件温和、官能团容忍性好和实验操作简单等特点。所得的α-氟代氰基酮还可以进行多种转化，从而得到各种氟代化合物。
