| Autor: |
Chalyk BA; Enamine Ltd., 78 Winston Churchill Street, Kyiv 02094, Ukraine.; Epiendo Pharmaceuticals, Sverige filial, Banvaktsvägen 22, 171 48 Solna, Stockholm, Sweden.; Institute of Organic Chemistry of the NAS of Ukraine, 5 Academician Kukharya Street, Kyiv 02094, Ukraine., Zginnyk O; Enamine Ltd., 78 Winston Churchill Street, Kyiv 02094, Ukraine., Khutorianskyi AV; Enamine Ltd., 78 Winston Churchill Street, Kyiv 02094, Ukraine., Mykhailiuk PK; Enamine Ltd., 78 Winston Churchill Street, Kyiv 02094, Ukraine. |
| Abstrakt: |
Electron-rich, electron-deficient, and non-activated alkenes can be rapidly functionalized by in situ -generated difluoromethyl nitrile oxide. The (3+2) cycloaddition proceeds at room temperature, has broad functional group tolerance, and can be used for the late-stage modification of bioactive molecules (finasteride and carbamazepine). The obtained CF 2 H-isoxazolines can be easily transformed into CF 2 H-containing building blocks for medicinal chemistry: amines, amino acids, amino alcohols, and spirocyclic scaffolds. |
