反应详情

A round-bottomed flask was charged with 2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid (110 mg, 0.25 mmol) and cis-tert-butyl 3-aminocyclobutylcarbamate (65 mg, 0.35 mmol). Then DMF (1.2 ml) was added followed by N,N-diisopropylethylamine (0.12 ml, 0.69 mmol) and HATU (104 mg, 0.27 mmol). The yellow reaction mixture was stirred at room temperature overnight then water and petroleum ether were added. The suspension was filtered and the solids were washed with water and a little petroleum ether. The product collected was dried under high vacuum to afford 145 mg (95%) of (cis-3-{[2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanylethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carbonyl]-amino}-cyclobutyl)-carbamic acid tert-butyl ester as an off-white powder.

1. filtrationThe suspension was filtered
2. washthe solids were washed with water
3. customThe product collected
4. customwas dried under high vacuum