反应详情

N-(3-(2,4-Dichlorophenyl)-2,6-dimethylpyrazolo[5,1-b]oxazol-7-yl) propionamide (634 mg, 1.800 mmol) is suspended in dry DMF (20 ml) and treated with NaH (60% in oil) (86 mg, 2.160 mmol) under N2 at RT. The mixture is stirred at RT for 10 minutes before cooling to 0° C. in an ice bath. 1-Iodopropane (0.263 ml, 2.70 mmol) is added dropwise and the reaction mixture is stirred at 0° C. for 1 hr. The solvent is removed in vacuo and the resulting residue is dissolved in EtOAc and washed with 1M NaOH, 1M HCl, H2O, brine, dried (MgSO4) and evaporated down to give a brown oil. Purification by chromatography on silica eluting with 0% to 50% EtOAc/iso-hexane affords the title compound as a clear oil; MS: m/z 394.1 [M+H]+

1. temperaturebefore cooling to 0° C. in an ice bath
2. stirringthe reaction mixture is stirred at 0° C. for 1 hr
3. customThe solvent is removed in vacuo
4. dissolutionthe resulting residue is dissolved in EtOAc
5. washwashed with 1M NaOH, 1M HCl, H2O, brine
6. dry with materialdried (MgSO4)
7. customevaporated down
8. customto give a brown oil
9. customPurification by chromatography on silica eluting with 0% to 50% EtOAc/iso-hexane