反应详情

250 mg (1.06 mmol) of 3-(1,6-dihydro-6-oxo-9H-purin-9-yl)propionic acid, ethyl ester (AIT-0027) was added to a 10 ml round bottom flask equipped with a magnetic stirring bar, reflux condenser, and a CaCL2 drying tube. 452 mg (3.18 mmol) 1-(3-aminopropyl)-2-pyrrolidinone and 1 ml acetonitrile were added. The solution was heated to reflux for 17 hours at which time all of the acetonitrile was evaporated leaving a dark viscous oil. The oil was chromatographed on 15 g silica gel, eluting with 40% methanol/60% ethyl acetate. This procedure gave 185 mg of 3-(1,6-dihydro-6-oxo-9H-purin-9-yl)-N-[3-(2-oxopyrrolidin-1-yl)propyl]propanamide (AIT-0034) as a pure white solid. Yield: 53%

1. customequipped with a magnetic stirring bar
2. temperaturereflux condenser
3. customa CaCL2 drying tube
4. temperatureThe solution was heated
5. customwas evaporated
6. customleaving a dark viscous oil
7. customThe oil was chromatographed on 15 g silica gel
8. washeluting with 40% methanol/60% ethyl acetate