反应详情

4-Chloro-1H-pyrrolo[2,3-d]pyrimidine (2.10 g, 13.6 mmol) was dissolved in 1-butanol (60.0 mL) and N,N-diisopropylethylamine (3.57 mL, 20.5 mmol) was added followed by (S)-(+)-1-aminoindan (1.93 mL, 15.0 mmol). The mixture was heated to reflux for 60 h, cooled down to rt and the solvent was evaporated to dryness. The residue was purified via silica gel chromatography eluting with a gradient of 0 to 100% EtOAc in DCM to afford the title compound (2.72 g, 80%). LC/MS: Rt=1.42 min, ES+ 251 (AA standard).

1. temperatureThe mixture was heated
2. temperatureto reflux for 60 h
3. customthe solvent was evaporated to dryness
4. customThe residue was purified via silica gel chromatography
5. washeluting with a gradient of 0 to 100% EtOAc in DCM