反应详情

温度

145 °C

Added to a solution of 0.8 g of methyl 7-bromo-1-oxo-2-(1-propylbutyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxylate in 8 cm3 of dioxane, under an argon atmosphere at a temperature close to 20° C. are 308 mg of tetrakis(triphenylphosphine)palladium and 3.2 g of 2-(tri-n-butylstannyl)oxazole. The reaction medium is heated at 145° C. in a microwave oven for 15 minutes, then left to return to a temperature close to 20° C. The reaction medium is concentrated to dryness under reduced pressure (5 kPa). The residue is taken up by 5 cm3 of dichloromethane and purified by flash chromatography over silica (column: 110 g; spherical silica of BP-SUP type particle size: 20-40 μm; eluent: 90% heptane/10% ethyl acetate then 100% ethyl acetate). After concentrating the fractions under reduced pressure, 320 mg of methyl 7-(2-oxazolyl)-1-oxo-2-(1-propylbutyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxylate are obtained.

1. customclose to 20° C.
2. waitleft
3. customclose to 20° C
4. concentrationThe reaction medium is concentrated to dryness under reduced pressure (5 kPa)
5. custompurified by flash chromatography over silica (column
6. concentrationAfter concentrating the fractions under reduced pressure, 320 mg of methyl 7-(2-oxazolyl)-1-oxo-2-(1-propylbutyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxylate
7. customare obtained