(3-METHOXY-PHENYLAMINO)-PHENYL-ACETIC ACID synthesis

Yield:725252-88-0 99%

Reaction Conditions:

Stage #1: 2-bromophenylacetic acid;m-Anisidinewith N-ethyl-N,N-diisopropylamine in tetrahydrofuran; for 4 h;Reflux;
Stage #2: with hydrogenchloride in water;

Steps:

26

A solution of 2-bromo-2-phenylacetic acid (0.5 g, 2.28 mmol) and 3- methoxyaniline (0.54 mL, 4.56 mmol) in THF (12 mL) is refluxed for 4 hours. Solvent is removed under vacuum, the residue is taken up with IM HCl and extracted with EtOAc. The organic phase is dried (Na₂SO₄), filtered and evaporated. The crude is purified by flash chromatography (DCM/MeOH=98/2 to 9/1) to obtain intermediate 1116 as a white solid (0.58 g, 99% yield).

References:

WO2010/72338,2010,A1 Location in patent:Page/Page column 96-97