Université de Strasbourg, Université de Haute-Alsace, CNRS, UMR 7042-LIMA, ECPM, 25 Rue Becquerel, Strasbourg 67087, France.
Bayer S.A.S., 14 Impasse Pierre Baizet, BP99163, 69263 Lyon Cedex 09, France.
Org Lett. 2020 Nov 6;22(21):8741-8745. doi: 10.1021/acs.orglett.0c03380. Epub 2020 Oct 22.
The functionalization of 3-(difluoromethyl)pyridine has been developed via direct deprotonation of -CHF with a lithiated base and subsequent trapping with various electrophiles in THF. quenching gives access to 3-pyridyl-CF-SiMePh as a new silylated compound, which can be postfunctionalized with a fluoride source to obtain a larger library of 3-(difluoroalkyl)pyridines that could not be accessed via direct deprotonation.
通过用锂化碱直接脱质子化 -CHF ,并随后在四氢呋喃中用各种亲电试剂捕获,开发了 3-(二氟甲基)吡啶的功能化。淬灭可得到 3-吡啶基-CF-SiMePh 作为一种新的硅化化合物,它可以用氟源进行后功能化,得到更大的 3-(二氟烷基)吡啶库,这些化合物无法通过直接脱质子化获得。