反应详情

A mixture of 2-chloro-5-(1-methyl-1H-1,2,4-triazol-3-yl)pyridine (3BX) (400 mg, 2.06 mmol); N-Tert-Butoxycarbonyl-1,2,3,6-tetrahydropyridine-4-boronic acid, pinacol ester (1.4 g, 4.53 mmol); Cesium carbonate (2.3 g, 7.07 mmol) and PdCl2dppf (100 mg) in dioxane/H2O (v/v 10:1, 20 ml) was stirred at 100° C. for 2 hours. The reaction was cooled, diluted with CH2Cl2 (300 ml) and H2O (100 ml), organic layer separated, dried over Na2SO4, filtered and solvent evaporated yielding a residue which chromatographed on silica gel eluting with EtOAc yielding title product 4BX as a solid (400 mg, 57%) MS (MH, 342).

1. temperatureThe reaction was cooled
2. customseparated
3. dry with materialdried over Na2SO4
4. filtrationfiltered
5. customsolvent evaporated
6. customyielding a residue which
7. customchromatographed on silica gel eluting with EtOAc yielding title product 4BX as a solid (400 mg, 57%)