反应详情

5-(3,3-Dimethylbut-1-yn-1-yl)-4-methylisoxazole-3-carboxylic acid (85 mg, 0.410 mmol) and 4-amino-2-cyclohexyl-1,5-dimethyl-1H-pyrazol-3(2H)-one (Intermediate D) (86 mg, 0.410 mmol) in DMF (2 mL) were treated with DIPEA (0.287 mL, 1.641 mmol) and HATU (172 mg, 0.451 mmol) at room temperature and stirred for 16 hours. The resulting mixture was diluted with water and extracted with EtOAc. The combined organic extracts were washed with a 0.5 M Lithium Chloride (aq) solution, dried over MgSO4, filtered and the solvent removed under reduced pressure. The crude material was adsorbed onto silica and purification by chromatography eluting with 0-100% EtOAc in iso-hexane afforded the title compound;

1. extractionextracted with EtOAc
2. washThe combined organic extracts were washed with a 0.5 M Lithium Chloride (aq) solution
3. dry with materialdried over MgSO4
4. filtrationfiltered
5. customthe solvent removed under reduced pressure
6. customThe crude material was adsorbed onto silica and purification by chromatography
7. washeluting with 0-100% EtOAc in iso-hexane