反应详情

1.5 g (5.2 mmol) of ethyl 8-methoxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate were dissolved in 90 mL of acetonitrile and 1.6 g (10.6 mmol) of sodium iodide and 1.5 mL of trimethylsilylchloride were added. After a day under stirring and nitrogen atmosphere at room temperature the solvent was evaporated, the residue redissolved with a mixture dichloromethane/methanol 4/1 and washed with a saturated aqueous solution of Na2S2O3. The organic layer was dried over Na2SO4 and evaporated to dryness. The residue crystallized from methanol leading 1.1 g of the title compound (78% yield).

1. customnitrogen atmosphere at room temperature the solvent was evaporated
2. dissolutionthe residue redissolved with a mixture dichloromethane/methanol 4/1
3. washwashed with a saturated aqueous solution of Na2S2O3
4. dry with materialThe organic layer was dried over Na2SO4
5. customevaporated to dryness