反应详情

To a solution of 2-cyclopropyl-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid (4-hydroxymethyl-tetrahydro-pyran-4-yl)-amide (0.15 g, 0.33 mmol) in CH2Cl2 (7.5 mL) was added trifluoroacetic acid (1.5 mL). The reaction mixture was stirred at room temperature overnight then concentrated. The residue was dissolved in MeOH (10 mL) and H2O (1 mL) and Et3N (2 mL) were added. The reaction mixture was stirred at room temperature overnight then concentrated. The residue was triturated with Et2O to afford 96 mg (92%) of 2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid (4-hydroxymethyl-tetrahydro-pyran-4-yl)-amide as an off-white solid. MS: (M+H)+=317; mp=294.0-296.0.

1. concentrationthen concentrated
2. dissolutionThe residue was dissolved in MeOH (10 mL)
3. additionH2O (1 mL) and Et3N (2 mL) were added
4. stirringThe reaction mixture was stirred at room temperature overnight
5. concentrationthen concentrated
6. customThe residue was triturated with Et2O