Arylated β-dicarbonyl compounds and process for the preparation thereof

摘要

The invention discloses a one pot process for the arylation of β-dicarbonyl compounds. Particularly, the present invention discloses transition-metal-free, chemo-selective, one pot process for the C-arylation of malonamide esters having Formula I at room temperature provide temperature range to obtain the arylated compounds of formula II with good yield, wherein the arylated compounds are selected from mono-arylated compound and di-arylated compound or mixture thereof.

主权项

1. A one pot, process for C-arylation of β-dicarbonyl compounds of Formula I at temperature in the range of 20 to 30° C. comprising the steps of:
i. reacting benzyne precursor with compound of formula I in the ratio ranging between 1:1 to 1:8 in presence of 0.5 to 5 molar concentration solvent, and fluoride source to obtain a reaction mixture; ii. concentrating reaction mixture as obtained in step (a) in vacuo followed by purifying to obtain compound of formula II yielding in the range of 40-97% wherein R1 and R2 is independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl; substituted or unsubstituted aryl;R3=Ar or H; andAr is selected from phenyl; halo substituted phenyl wherein halo group is selected from fluro, chloro or bromo; alkyl substituted phenyl wherein alkyl is selected from methyl, ethyl, propyl or butyl.