Reacción #665

ord-bd4700a79525457dbcfd3c5e1368118f

Ecuación de reacción

Brc1ccccc1
Brc1ccccc1
c1ccc(C2CCCCN2)cc1
c1ccc(C2CCCCN2)cc1
c1ccc(C2CCCCN2c2ccccc2)cc1
c1ccc(C2CCCCN2c2cccc
Rendimiento 15.6%

Disolventes

Condiciones de reacción

Temperatura
100°CELSIUS

Procedimiento

Caesium carbonate (556 mg, 1.71 mmol) was added to bromobenzene (0.060 mL, 0.57 mmol) and 2-phenylpiperidine (110 mg, 0.68 mmol) in 1,4-dioxane (2 mL). The reaction was degassed and Tris(dibenzylideneacetone)?dipalladium(0) (13.01 mg, 0.01 mmol) and dicyclohexyl(2',6'-diisopropoxy-[1,1'-biphenyl]-2-yl)phosphine (RuPhos) (13.26 mg, 0.03 mmol) were added. The resulting solution was stirred at 100 °C for 16 hours. LCMS showed The reaction mixture was diluted with EtOAc, and washed with water. The organic layer was dried over MgSO4, filtered and evaporated to afford crude product. The crude product was purified by flash silica chromatography, elution gradient 0 to 15% MeOH in DCM. Pure fractions were evaporated to dryness to afford 1,2-diphenylpiperidine (21.00 mg, 15.56 %) as a yellow oil. f0 = 19 mg bromobenzene f1 = 21 mg product The reaction was abandonned.

Fuente

750 AstraZeneca ELN dataset