Reaktion #492

ord-ff0eb93bbb4b45cdb3807c4588dd206f

Reaktionsgleichung

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)
Ausbeute 78.2%

Lösungsmittel

Reaktionsbedingungen

Temperatur
100°CELSIUS

Vorschrift

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 %)

Quelle

750 AstraZeneca ELN dataset