反应详情

温度

100 °C

To a solution of [bis-(4-methoxy-phenyl)-phenyl-methyl]-[(2R,5R)-5-(6-bromo-3-fluoro-pyridin-2-yl)-2,5-dimethyl-2-trifluoromethyl-5,6-dihydro-2H-[1,4]oxazin-3-yl]-amine (250 mg, 0.372 mmol) in toluene (3.72 ml) was added 2-amino-3-pyridinecarbonitrile (221 mg, 1.859 mmol), Pd2(dba)3 (6.81 mg, 7.43 μmol), BINAP (9.26 mg, 0.015 mmol) and sodium tert-butoxide (50 mg, 0.520 mmol). The reaction mixture was degassed for 5 min and the microwave vial was sealed and stirred at 100° C. for 9 h. The reaction mixture was diluted with DCM and washed with water. The organic layer was dried with Na2SO4. The residue was purified by chromatography (silica gel; eluent DCM/MeOH+NH4OH) to afford the title compound.

1. customThe reaction mixture was degassed for 5 min
2. customthe microwave vial was sealed
3. additionThe reaction mixture was diluted with DCM
4. washwashed with water
5. dry with materialThe organic layer was dried with Na2SO4
6. customThe residue was purified by chromatography (silica gel; eluent DCM/MeOH+NH4OH)