反应详情

温度

80 °C

To a de-gassed mixture of 4-[6-chloro-4-(3-chloro-4-fluoro-phenyl)pyridin-2-yl]-morpholine (50 mg, 0.153 mmol)), 5-chloro-6-piperazin-1-yl-nicotinic acid ethyl ester (0.183 mmol), and 1M (THF) t-BuOK (0.183 mmol), in toluene (3 mL) under nitrogen add Pd2(dba)3 (0.006 mmol) and BINAP (0.008 mmol). Stir the mixture at 80° C. for 16 h, concentrate, and extract with EtOAc. Dry over Na2SO4, concentrate under vacuum, and purify by preparative TLC (3:1 hexanes/EtOAc) to give the title ester.

1. concentrationconcentrate
2. extractionextract with EtOAc
3. dry with materialDry over Na2SO4
4. concentrationconcentrate under vacuum
5. custompurify by preparative TLC (3:1 hexanes/EtOAc)