反应详情

Heat a solution of trifluoro-methanesulfonic acid 3,5-dichloro-4-[trans-1-(4-fluoro-cyclohexyl)-2-oxo-pyrrolidin-3-ylmethyl]-phenyl ester (Preparation 28) (0.346 g, 0.705 mmol), pyridine-3-boronic acid (0.173 g, 1.41 mmol), Pd(PPh3)4 (81 mg), 7 mL of 0.1 M Na2CO3 aq solution in 7 mL of dimethoxy ethane at 80° C. for 24 h. Cool the mixture to room temp and dilute with 20 mL of 1N NaHCO3. Dilute the mixture with 20 mL of EtOAc. Wash the organic layer with water, brine and dry over Na2SO4, filter and concentrate. Purify the crude material by chromatography to afford the title compound: mass spectrum (m/z): 421 (M+1).

1. washWash the organic layer with water, brine
2. dry with materialdry over Na2SO4
3. filtrationfilter
4. concentrationconcentrate
5. customPurify the crude material by chromatography