反应详情

Add 87 mg (2.16 mmol) sodium hydride (60% dispersion in mineral oil) to a solution of 350 mg (1.73 mmol) (6R)-6-hydroxyheptanoic acid tert.-butyl ester in 5 ml THF, with ice cooling. After stirring for ten minutes with ice cooling, add a solution of 644 mg (1.82 mmol) 4-chloro-6-(2-fluorophenyl)-5-(4-methoxyphenyl)furo[2,3-d]pyrimidine in 5 ml THF and 32 mg (0.09 mmol) tetra-n-butylammonium iodide. Stir the reaction mixture for 48 h at RT. After adding water and ethyl acetate, wash the separated organic phase with 1 N hydrochloric acid and concentrate by vacuum evaporation. Take up the residue in acetonitrile/DMSO and purify by preparative RP-HPLC (gradient: water/acetonitrile). 425 mg (47% of theor.) of the desired product is obtained.

1. stirringStir the reaction mixture for 48 h at RT
2. washwash the separated organic phase with 1 N hydrochloric acid
3. concentrationconcentrate by vacuum evaporation
4. custompurify by preparative RP-HPLC (gradient: water/acetonitrile)