Diisopropylethylamine → 1-[1-(3-Chloro-4-fluoro-phenyl)-5-(5-fluoro-3-pyridyl)pyrazole-3-carbonyl]imidazolidin-4-one

Participants

Reaction Steps

0.16 ml (0.89 mmol) of N,N-diisopropylethylamine is added to a solution of 100 mg (0.30 mmol) of the compound of Example 60A, 40 mg (0.33 mmol) of 4-imidazolinone-hydrochloride, and 217 mg (0.42 mmol) of PYBOP in 2 ml of THF, and the mixture that is obtained is stirred for 16 hours at room temperature. The reaction mixture is concentrated by evaporation in a vacuum. The residue is diluted with acetonitrile, filtered over a Millipore spray filter, and separated by means of preparative HPLC (mobile solvent: acetonitrile/water gradient). Solvent is removed from the product-containing fractions in a rotary evaporator, and the residue is recrystallized from acetonitrile. 96 mg (80% of theory) of the title compound is obtained.

Provenance & Evidence