反应详情

This was generated via the cyclization of known intermediate 1-(2,3-difluorobenzyl)-5-(isoxazol-3-yl)-1H-pyrazole-3-carboximidamide (213 mg, 0.702 mmol) with sodium 3-ethoxy-2-fluoro-3-oxoprop-1-en-1-olate (440 mg, 2.81 mmol) in ethanol (5.0 mL)—stirring at 90° C. for 14 hour. The solvent was removed in vacuo, and purification by silica gel chromatography (0-10% methanol in DCM) provided a mixture of the desired compound and a side-product. The mixture was then subjected to reverse-phase preparative HPLC which afforded Compound 93 (15 mg, 7.2% yield) as a white solid.

1. customThe solvent was removed in vacuo, and purification by silica gel chromatography (0-10% methanol in DCM)
2. customprovided