反应详情

温度

70 °C

6-Bromo-4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-(phenylsulfonyl)-1H-indazole (300 mg, 0.661 mmol) and sodium iodide (138 mg, 0.921 mmol) were weighed into a round-bottomed flask and dissolved in acetonitrile (2 ml) before 1-amino-3-morpholin-4-ylpropan-2-ol (212 mg, 1.322 mmol, available from Enamine Ltd) and DIPEA (0.231 ml, 1.322 mmol) were added. The mixture was heated to 70° C. for 2 h, then cooled, diluted with DCM and washed with 2 M aqueous HCl (5 ml). The organic layer was separated with a hydrophobic frit and the aqueous layer was neutralised to pH 7 by addition of 2M NaOH resulting in the formation of a solid precipitate. This was filtered off under vacuum and dried in air for 2 h to give the title compound as a cream solid (220 mg).

1. additionwere added
2. temperaturecooled
3. washwashed with 2 M aqueous HCl (5 ml)
4. customThe organic layer was separated with a hydrophobic frit
5. additionthe aqueous layer was neutralised to pH 7 by addition of 2M NaOH resulting in the formation of a solid precipitate
6. filtrationThis was filtered off under vacuum
7. customdried in air for 2 h