反应详情

A solution of 4-fluoro-1H-pyrrolo[2,3-c]pyridine-7-carboxylic acid ethyl ester (50 mg, 0.24 mmol) in THF (0.7 mL) was treated with 2 M aq. potassium hydroxide solution (0.24 mL, 0.48 mmol) and stirred for 90 min at RT. The reaction mixture was then evaporated, the residue dissolved in DMF (3.2 mL) and treated with (4-tert-butyl-benzyl)-[2-(4-chloro-3-trifluoromethyl-phenyl)-ethyl]-amine (98 mg, 0.26 mmol), N-methylmorpholine (73 mg, 0.72 mmol), and HBTU (137 mg, 0.36 mmol). After 16 h, the reaction mixture was partitioned between water and ethyl acetate, the organic layer was washed with brine, dried (MgSO4), and evaporated. Chromatography of the residue (SiO2, heptane/ethyl acetate 97:3) afforded the title compound (95 mg, 74%). White foam, MS (ISP) 532.3 (M+H)+.

1. customThe reaction mixture was then evaporated
2. dissolutionthe residue dissolved in DMF (3.2 mL)
3. waitAfter 16 h
4. customthe reaction mixture was partitioned between water and ethyl acetate
5. washthe organic layer was washed with brine
6. dry with materialdried (MgSO4)
7. customevaporated