反应详情

A mixture of (S)-ethyl 2-(5-bromo-4-(4,4-dimethylpiperidin-1-yl)-2,6-dimethylpyridin-3-yl)-2-(tert-butoxy)acetate (0.049 g, 0.108 mmol), (4-((4-fluorobenzyl)oxy)phenyl)boronic acid (0.040 g, 0.161 mmol) and 2M Na2CO3 (0.134 ml, 0.269 mmol) in DMF (2 mL) was degassed for 10 min. Then, Pd(Ph3P)4 (0.012 g, 10.76 μmol) was added, degassed for 5 min and placed in a pre-heated oil bath at 100° C. After 1.5 h at 110° C., cooled and purified by prep-HPLC to afford (S)-ethyl 2-(tert-butoxy)-2-(4-(4,4-dimethylpiperidin-1-yl)-5-(4-((4-fluorobenzyl)oxy)phenyl)-2,6-dimethylpyridin-3-yl)acetate (0.0372 g, 0.065 mmol, 59.9% yield) as tan color solid. LCMS (M+H)=577.6.

1. customwas degassed for 10 min
2. customdegassed for 5 min
3. customplaced in a pre-heated oil bath at 100° C
4. temperaturecooled
5. custompurified by prep-HPLC