Reaction #7744

Reaction equation

2-(4-fluorophenyl)-1-[4-morpholin-4-yl-2-(2-phenoxy-pyrimidine-4-carbonyl)pyrazolidine-1-yl]ethanone

NaH

→

desired product

Yield 20.0%

2-(4-fluorophenyl)-6-morpholin-4-yl-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-one

Yield 20.0%

Solvents

DMF

Conditions

Workup

1. 1
   OtherThe solvent is removed in vacuo the residue
2. 2
   workup.DISSOLUTIONdissolved in methylene chloride
3. 3
   Extractionextracted with water
4. 4
   Otherdried
5. 5
   Concentrationre-concentrated

Procedure

To a solution of 2-(4-fluorophenyl)-1-[4-morpholin-4-yl-2-(2-phenoxy-pyrimidine-4-carbonyl)pyrazolidine-1-yl]ethanone, 19, (0.2 g, 0.4 mmol) in DMF (10 mL) at 0° C. is added NaH (0.024 g, 0.6 mmol) and the resulting solution is stirred 2 hours. The solvent is removed in vacuo the residue dissolved in methylene chloride and extracted with water, dried, and re-concentrated to afford 37 mg (20% yield) of the desired product as a yellow solid.

Source