反应详情

To a solution of 5-amino-4-(2-fluoro-4-iodo-phenylamino)-6-methoxy-indazole-1-carboxylic acid tert-butyl ester (200 mg, 0.401 mmol) in pyridine (2 mL) was added cyclopropyl sulfonyl chloride (281 mg, 2.0 mmol) and the reaction mixture stirred at room temperature for 18 hours. The reaction mixture was treated with water and extracted twice with ethyl acetate. The combined organic extracts were washed with water, dried (Na2SO4), filtered and concentrated in vacuo to give an oily residue. The residue was subjected to flash chromatography (Si—PPC, gradient 0 to 25% ethyl acetate in cyclohexane) to give the title compound as an off-white foam (217 mg, 89%). LCMS (Method B) RT=4.16 min, [M+H]+=603.

1. extractionextracted twice with ethyl acetate
2. washThe combined organic extracts were washed with water
3. dry with materialdried (Na2SO4)
4. filtrationfiltered
5. concentrationconcentrated in vacuo
6. customto give an oily residue