With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.
A mixture of Intermediate B (879 mg, 3.30 mmol), 4,4-difluoropiperidine (400 mg, 3.30 mmol), Pd2(dba)3 (302 mg, 0.330 mmol), xantphos (382 mg, 0.660 mmol) and KO’Bu (748 mg, 6.60 mmol) in toluene (10 ml) was bubbled with argon for 10 min. The mixture was then heated at 100¡ãC for overnight. The reaction was quenched with 60percent NaHC03 aqueous solution. The aqueous phase was extracted with DCM/IPA (20 ml x3, V/V = 3/1 ). The combined organic phase was dried over anhydrous MgS04. Filtered and concentrated. The residue was purified by silica gel chromatography (eluted with 2percent MeOH in DCM) to give the title compound as yellow solid (270 mg, 31 percent yield). LCMS (method B): [M+H]+ = 265, tR = 1.79 min.
21987-29-1, 21987-29-1 4,4-Difluoropiperidine 2758352, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; NOVARTIS AG; CHEN, Chao; DENG, Haibing; GUO, Haibing; HE, Feng; JIANG, Lei; LIANG, Fang; MI, Yuan; WAN, Huixin; XU, Yao-Chang; YU, Hongping; ZHANG, Ji Yue (Jeff); WO2013/38362; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem