1,2,3,4,7,8,9,9a-octahydropyrido[1,2-a]pyrazin-6-one

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of octahydro-pyrido[1,2-a]pyrazin-6-one (compound of Description 12, 20 mg, 0.13 mmol) in DCM (1 ml), TEA (16 mg, 0.16 mmol) and a solution of 2-fluoro-benzenesulfonyl chloride (25 mg, 0.13 mmol) in CH3CN (1 ml) were added at 0° C. After stirring 3 hours at room temperature, the solvent was evaporated. The residue was partitioned between water and ethyl acetate. The organic layer was washed with brine, dried (Na2SO4) and evaporated under reduced pressure. The residue was purified by flash chromatography (from DCM to DCM/MeOH/32% NH4OH 95/5/0.5 respectively) to afford the title compound (18 mg, 44% yield). the solvent was evaporated The residue was partitioned between water and ethyl acetate The organic layer was washed with brine dried (Na2SO4) evaporated under reduced pressure The residue was purified by flash chromatography (from DCM to DCM/MeOH/32% NH4OH 95/5/0.5 respectively)

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 4-Pyrazin-2-yl-butyric acid ethyl ester (1 g, 5.14 mmol) was dissolved in abs. EtOH (50 ml) and hydrogenated over 10% Pd/C (200 mg) at 50 psi for 20 hours. After filtration, the solvent was removed under vacuum and the residue was purified by flash chromatography (DCM/MeOH/32% NH4OH from 95/5/0.5 to 90/10/1 respectively) to afford the title compound (454 mg, 57% yield). After filtration the solvent was removed under vacuum the residue was purified by flash chromatography (DCM/MeOH/32% NH4OH from 95/5/0.5 to 90/10/1 respectively)