Reference of 134227-45-5, These common heterocyclic compound, 134227-45-5, name is 3,4,5-Trifluorobenzonitrile, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
A mixture of 8-(pirhoeridin-3-ylacetyl)-8-azabicyclo[3.2.1]octan-3-ol hydrochloride (0.035 g, 0.00012 mol), 3,4,5-trifiuorobenzonitrile (0.0209 g, 0.000133 mol) and potassium carbonate (0.0419 g, 0.000303 mol) in N,N-dimethylformamide (0.700 mL, 0.00904 mol) was heated at 100 0C overnight. After quenched with water, the mixture was extracted with EtOAc. The organic layers were combined, washed with water and brine successively, dried, and evaporated to dryness. The residue was purified on RP-HPLC to give the desired product (36 mg 77%). LCMS (M+H) 390.2. The product was believed to have a 3-endo configuation based on the starting materials.
Statistics shows that 3,4,5-Trifluorobenzonitrile is playing an increasingly important role. we look forward to future research findings about 134227-45-5.
Reference:
Patent; INCYTE CORPORATION; WO2007/89683; (2007); A1;,
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts