反应详情

2-Furan-2-yl-5-methanesulfonyl-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-ylamine (2.5 mmol; see Example 1(a)) was suspended in 20 mL of CH3CN along with 5 mmol of (R)-2-aminomethyl-1-Boc-pyrrolidine (Astatech, Monmouth Junction, N.J.). The reaction mixture was stirred under reflux for 2 hours. It was then cooled to room temperature and concentrated under reduced pressure. The resulting residue was diluted with CH2Cl2 and washed with dilute 1% citric acid, brine, dried with Na2SO4 and concentrated under reduced pressure. Purification by chromatography (98% CH2Cl2, 2% MeOH) afforded 880 mg of 2-[(7-amino-2-furan-2-yl-[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-ylamino)-methyl]-pyrrolidine-1-carboxylic acid tert-butyl ester.

1. temperatureunder reflux for 2 hours
2. concentrationconcentrated under reduced pressure
3. additionThe resulting residue was diluted with CH2Cl2
4. washwashed
5. additionwith dilute 1% citric acid, brine
6. dry with materialdried with Na2SO4
7. concentrationconcentrated under reduced pressure
8. customPurification by chromatography (98% CH2Cl2, 2% MeOH)