Yield:-

Reaction Conditions:

with sodium carbonate in water;

Steps:

4.A

The HCl salt of (S_y)-l-(2,4-difluorophenyl)-ethylamine was treated with aq Na2CO3. Repeated extraction with DCM followed by concentration provided the freebase, which was transferred directly in NMP (6 mL) for use in this reaction. To this solution was added 7a (240 mg) and the resulting solution was heated in a sealed vial at 220 ⁰C for 15 min with microwave irradiation. The reaction mixture was diluted with EtOAc and was repeatedly washed with water and brine. The organic layer was dried, filtered and concentrated. Flash chromatography (SiC^, 0-20% MeOH/DCM gradient) provided 8aa as a pale yellow solid (275 mg, 0.75 mmol, 75% yield).

References:

WO2009/85913,2009,A1 Location in patent:Page/Page column 75