反应详情

A solution of tert-butyl(trans)-2-(4-bromophenyl)cyclopropylcarbamate (Intermediate F; 1 equiv), 1.2 equiv of the boronic acid, 3.0 equiv of K2CO3 in CH3CN+H2O (4:1) was degassed for 30 mins with Argon gas, added 0.01 equiv of Pd (PPh3)4, heated the reaction mixture at reflux temp for 4 h. The progress of the reaction was monitored by TLC, after completion, poured the reaction mixture into water, extracted with EtOAc. The combined extracts were washed with water, brine, dried over anhydrous Na2SO4, filtered and evaporated. The crude residue was purified by column chromatography to get tert-butyl(trans)-2-(1,1′-biphenyl-4-yl)cyclopropylcarbamate derivative

1. temperatureheated the reaction mixture
2. temperatureat reflux temp for 4 h
3. extractionextracted with EtOAc
4. washThe combined extracts were washed with water, brine
5. dry with materialdried over anhydrous Na2SO4
6. filtrationfiltered
7. customevaporated
8. customThe crude residue was purified by column chromatography