反应详情

To a suspension of 2-methyl-8,9,10,10a-tetrahydropyrido[2′,3′:3,4]pyrrolo[1,2-a]pyrazin-5(7H)-one (may be prepared as described in Intermediate 8; 70 mg) in DCM (5 mL) was added DIPEA (0.241 mL, 1.378 mmol). To this was added 4-(ethyloxy)benzenesulfonyl chloride (80 mg) and this was allowed to stir at room temperature for 30 minutes. The reaction mixture was partitioned between DCM and saturated sodium bicarbonate solution in a hydrophobic frit. The aqueous layer was re-extracted with DCM. The combined organic phases were evaporated to an orange oil. The residue was purified by chromatography (25S silica cartridge) eluting with 0-5% methanol in DCM over 12 column volumes. The clean fractions were combined and evaporated to give the title compound as a white foam (84 mg).

1. customThe reaction mixture was partitioned between DCM and saturated sodium bicarbonate solution in a hydrophobic frit
2. extractionThe aqueous layer was re-extracted with DCM
3. customThe combined organic phases were evaporated to an orange oil
4. customThe residue was purified by chromatography (25S silica cartridge)
5. washeluting with 0-5% methanol in DCM over 12 column volumes
6. customevaporated