Duolip,Merckle,W. Germany,1981
Cardiac analeptic;Phosphodiesterase inhibitor
Useful synthetic intermediate in the preparation of 7-substituted xanthines.
An inhibitor of 3’,5’-Cyclic Nucleotide Phosphodiesterase. Therapeutically, this compound has diuretic, muscle relaxant, bronchial dilation and CNS stimulant activities.
ChEBI: 7-(2-hydroxyethyl)-1,3-dimethylpurine-2,6-dione is an oxopurine.
107.3 g (0.5 mol) 2-(p-chlorophenoxy)isobutyric acid and 56.0 g (0.25 mol)
7-hydroxyethyltheophylline were suspended together in 250 ml xylene. They
were heated together for 15 hours in a water separator following the addition
of 1.5 g p-toluenesulfonic acid. The solution was next agitated with dilute
sodium bicarbonate solution (0.5 mol NaHCO3), water washed and evaporated
in a rotary evaporator.
The residue was then crystallized from isopropanol, yielding 58.0 g (55%
yield) of 1-(7-theophyllinyl)-2-ethyl[2-(p-chlorophenoxy)-isobutyrate] . The
compound had a melting point of 131°C to 132°C.
Pharmacological profile similar to theophylline.
