反应 #1880981

反应方程式

Et3N

(4S,2R,5R)-2-[6-(cyclopentylamino)purin-9-yl]-5-prop-2-ynyloxolane-3,4-diol

1-fluoro-2-iodobenzene

→

(4S,2R,3R,5R)-2-[6-(cyclopentylamino)purin-9-yl]-5-[3-(2-fluorophenyl)prop-2-ynyl]oxolane-3,4-diol

溶剂

THF

反应条件

后处理

1. 1
   其他The solvent was removed under reduced pressure
2. 2
   其他the residue was purified by preparative thin layer chromatography

实验过程

To a stirred solution of (4S,2R,5R)-2-[6-(cyclopentylamino)purin-9-yl]-5-prop-2-ynyloxolane-3,4-diol (0.017 g, 0.05 mmol) and 1-fluoro-2-iodobenzene (0.02 mL, 0.13 mmol) in THF (3.50 mL) under an atmosphere of N2 was added catalytic amount of dichlorobis(triphenylphosphine) palladium (II) and copper (I) iodide. Et3N (0.20 mL) was then added. The resulting mixture was stirred under N2 at 75° C. for 2 days. The solvent was removed under reduced pressure, and the residue was purified by preparative thin layer chromatography to give (4S,2R,3R,5R)-2-[6-(cyclopentylamino)purin-9-yl]-5-[3-(2-fluorophenyl)prop-2-ynyl]oxolane-3,4-diol, a compound of Formula I.

来源