反应详情

248 mg (1.0344 mmol) of 4-[(2-aminoethyl)amino]-2-hydroxy-4-oxo-N,N,N-trimethyl-1-butanaminium chloride was placed into a 10 ml round bottom flask with magnetic stirring bar. Then 2 ml of dimethylsulfoxide was added and the solution was gently heated to help dissolve the amine. 340 mg (1.034 mmol) of 3-(1,6-dihydro-6-oxo-9H-purin-9-yl)propanoic acid, 4-nitrophenyl ester (AIT-0081) was added to the stirring solution. The solution was stirred for a period of one hour and 3 ml of methanol was added. Then 3 ml of acetone was added and the solution was filtered. The solid was washed several times with acetone and allowed to dry. This yielded 105 mg of 4-[[2-[[3-(1,6-dihydro-6-oxo-9H-purin-9-yl)-1-oxopropyl]amino]ethyl]amino]-2-hydroxy-4-oxo-N,N,N-trimethyl-1-butanaminium chloride (AIT-0090) as a white solid. m.p. approximately 260-265 (dec) Yield: 33%.

1. temperaturethe solution was gently heated
2. filtrationthe solution was filtered
3. washThe solid was washed several times with acetone
4. customto dry