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2,4,6-trichloro-8-fluoro-7-(2-fluoro-6-methoxyphenyl)quinazoline[ No CAS ]
(2R,5S)-tert-butyl 4-(2,6-dichloro-8-fluoro-7-(2-fluoro-6-methoxyphenyl)quinazolin-4-yl)-2,5-dimethylpiperazine-1-carboxylate[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
2.1 g
With triethylamine; In dichloromethane; at 0 - 20℃;
To a stirred solution of 2,4,6-trichloro-8-fluoro-7-(2-fluoro-6- methoxyphenyl)quinazoline (2 g, 5.34 mmol) in DCM (2OmL) at 0 °C, TEA (1.08 g, 10.7 mmol) was added and then (2R,5S)-tert-butyl 2,5-dimethylpiperazine-1- carboxylatet (1.15 g, 5.34 mmol) in DCM (20 mL) was added slowly. The mixture was stirred at RT overnight. The mixture was partitioned between water (5OmL) and DCM(lOOmL X 2).The organic layer was concentrated in vacuo and the residue was purified by flash column chromatography on silica gel to afford the desired product 3-2 (2.1 g). ESI-MS m/z: 553 [M+H].
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