反应详情

温度

90 °C

A mixture of 9-{[2-bromo-4-(trifluoromethyl)phenyl]sulfonyl}-8,9,10,10a-tetrahydropyrido[2′,3′:3,4]pyrrolo[1,2-a]pyrazin-5(7H)-one (265 mg; may be prepared as described in Intermediate 24), trimethylboroxin (182 mg), potassium carbonate (200 mg) and Pd(PPh3)4 (109 mg) was heated to 90° C. under argon for 6 hours. The reaction mixture was partitioned between EtOAc and saturated sodium bicarbonate solution, and then the aqueous was re-extracted with EtOAc. The combined organic phases were washed with brine, dried through a hydrophobic frit and evaporated to a brown oil (335 mg). The residue was purified by chromatography eluting with 0-90% ethyl acetate in iso-hexane over 12 column volumes. The desired fractions were combined and evaporated to give the title compound as a pale yellow crystalline solid (128 mg).

1. customThe reaction mixture was partitioned between EtOAc and saturated sodium bicarbonate solution
2. extractionthe aqueous was re-extracted with EtOAc
3. washThe combined organic phases were washed with brine
4. customdried through a hydrophobic frit
5. customevaporated to a brown oil (335 mg)
6. customThe residue was purified by chromatography
7. washeluting with 0-90% ethyl acetate in iso-hexane over 12 column volumes
8. customevaporated