反应详情

A mixture of methyl 2-(1-methyl-6-(trifluoromethyl)-1H-indazol-3-yl)-5-(pivaloyl oxymethyl)-5H-pyrrolo[3,2-b]pyrazine-7-carboxylate (200 mg, 0.409 mmol) and KOH (229 mg, 4.09 mmol) in 1,4-dioxane (5 mL) and water (2 mL) was heated to reflux for 4 hours. Dioxane was concentrated and the residual aqueous layer was adjusted to pH=4 with 1.0 M HCl. The precipitate was collected by filtration and dried to afford 2-(1-methyl-6-(trifluoromethyl)-1H-indazol-3-yl)-5H-pyrrolo[3,2-b]pyrazine-7-carboxylic acid (230 mg, crude) as a yellow solid. LCMS: (M+H)+=362.

1. temperaturewas heated
2. temperatureto reflux for 4 hours
3. concentrationDioxane was concentrated
4. filtrationThe precipitate was collected by filtration
5. customdried