Reacción #492

ord-ff0eb93bbb4b45cdb3807c4588dd206f

Ecuación de reacción

COC(=O)c1cc(Br)cc(C(=O)OC)c1
COC(=O)c1cc(Br)cc(C(
C1COCCN1
C1COCCN1
COC(=O)c1cc(C(=O)OC)cc(N2CCOCC2)c1
COC(=O)c1cc(C(=O)OC)
Rendimiento 78.2%

Disolventes

Condiciones de reacción

Temperatura
100°CELSIUS

Procedimiento

To a solution of dimethyl 5-bromoisophthalate (10 g, 36.62 mmol) in toluene (100 mL) where BINAP (2.5 g, 4.01 mmol), morpholine (4.4 g, 50.50 mmol), CESIUM CARBONATE (18 g, 55.25 mmol) and PALLADIUM(II) ACETATE (0.9 g, 4.01 mmol) added. The solution was heated to reflux under inert atm for 14h. The silvent was filtered and the filtrate was concentrated. The residue was purified by column chropmatography (Hep:EA) 1:1 to give dimethyl 5-morpholinoisophthalate (8.00 g, 78 %)

Fuente

750 AstraZeneca ELN dataset