反应详情

温度

0 °C

In a round-bottomed flask, 2-[5-(tert-butyl-dimethyl-silanyloxymethyl)-1-methyl-1H-indazol-3-yl]-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid isopropylamide (425 mg, 0.66 mmol) was dissolved in THF (6 ml). The light yellow solution was cooled to 0° C. and tetrabutylammonium fluoride (1.0 M in THF, 0.24 ml, 0.240 mmol) was added dropwise. The reaction mixture was allowed to warm slowly to room temperature over 2 h then quenched with water and extracted with EtOAc (2×). The combined organic layers were washed with water and brine then concentrated. The residue was triturated with diethyl ether to afford 2-(5-hydroxymethyl-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid isopropylamide as a yellow powder which was used without further purification.

1. temperatureto warm slowly to room temperature over 2 h
2. customthen quenched with water
3. extractionextracted with EtOAc (2×)
4. washThe combined organic layers were washed with water and brine
5. concentrationthen concentrated
6. customThe residue was triturated with diethyl ether