反应详情

A 2-5 ml microwave vial is charged with Pd(OAc)2 (2.5 mol %, 4.1 mg, 0.016 mmol), Xantphos (5 mol %, 24.9 mg, 0.0321 mmol), ureido-acetic acid tert-butyl ester (190.3 mg, 1.03 mmol), and Cs2CO3 (578.9 mg, 1.605 mmol). 2-Chloro-4-iodo-nicotinic acid ethyl ester (208.9 mg, 0.642 mmol) is added followed by 1,4-dioxane (4 ml). The vessel is sealed and treated in the microwave at 120° C. for 3600 seconds. EtOAc is added to the mixture, washed with brine (3×20 ml), then water (2×20 ml). The organic portions are passed through Celite® and the solvent removed in vacuo. The crude material is taken up in a minimal amount of DCM and loaded onto a 10 g Isolute™ pre packed Silica II cartridge, eluted with 100% iso-hexane to 50% EtOAc:Isohexane to afford the title compound; [M+H]+ 312

1. customThe vessel is sealed
2. additiontreated in the microwave at 120° C. for 3600 seconds
3. washwashed with brine (3×20 ml)
4. customthe solvent removed in vacuo
5. washeluted with 100% iso-hexane to 50% EtOAc