反应详情

2-Fluoro-benzenesulfonyl chloride (68.9 mg, 035 mmol) was added to a solution of (4-Amino-7-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-(2-amino-6-methyl-pyridin-4-yl)-methanone (100 mg, 0.32 mmol) in pyridine (2 mL). The mixture was stirred for 2 h at room temperature. The reaction mixture was quenched with H2O (2 mL) and concentrated in vacuo. The resulting residue was triturated with MeOH, filtered, and dried. Purification by flash column chromatography [ethyl acetate/hexanes 3:7—(20% NH4OH/MeOH)/ethyl acetate/hexanes 5:65:30] afforded the title compound as a yellow oil (94 mg, 62%). MS: 469.3 (MH+); HPLC Rf: 4.46 min. (HPLC method 4).

1. customThe reaction mixture was quenched with H2O (2 mL)
2. concentrationconcentrated in vacuo
3. customThe resulting residue was triturated with MeOH
4. filtrationfiltered
5. customdried
6. customPurification by flash column chromatography [ethyl acetate/hexanes 3:7—(20% NH4OH/MeOH)/ethyl acetate/hexanes 5:65:30]