反应详情

Couple 3′-chloro-2,3,5,6-tetrahydro-[1,2′]bipyrazinyl-4-carboxylic acid t-butyl ester (0.726 g, 2.43 mmol) and 4-ethoxyphenylboronic acid (0.95 g, 5.991 mmol), in the presence of triphenylphosphine (0.202 g, 0.770 mmol), palladium acetate (0.056 g, 0.243 mmol), sodium carbonate (3.8 mL of a 2 N solution in water) in a mixture of acetonitrile (42 mL) and water (8 mL). Reflux for 3 hr. Purify by silica gel chromatography, eluting with 0:100 to 25:75 ethyl acetate:hexanes, to give 3′-(4-ethoxyphenyl)-2,3,5,6-tetrahydro-[1,2′]bipyrazinyl-4-carboxylic acid t-butyl ester (1.79 g, 96%).

1. temperatureReflux for 3 hr
2. customPurify by silica gel chromatography
3. washeluting with 0:100 to 25:75 ethyl acetate