反应详情

To a solution of 4-iodo-2-methylsulfanyl-pyrimidine (390 mg, 1.56 mmol), 2,4-dimethyl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-thiazole (633 mg, 2.65 mmol added portionwise), Na2CO3 (215 mg, 2.02 mmol), triphenylphosphine (42 mg, 0.15 mmol) in nPrOH (25 ml), Pd(OAc)2 (11 mg, 0.047 mmol) was added and the mixture was refluxed for 2 hour. The solvent was evaporated under vacuum, and the crude was dissolved in DCM and washed with water. The organic phase was dried (Na2SO4) and evaporated. A second batch of this compound was prepared according to the same protocol starting from 0.39 mmol of 4-iodo-2-methylsulfanyl-pyrimidine. The residues, deriving from the two batches, were purified by flash chromatography with hexane-ethyl acetate to give the title compound (352, 76% yield).

1. additionwas added
2. temperaturethe mixture was refluxed for 2 hour
3. customThe solvent was evaporated under vacuum
4. dissolutionthe crude was dissolved in DCM
5. washwashed with water
6. dry with materialThe organic phase was dried (Na2SO4)
7. customevaporated
8. customA second batch of this compound was prepared
9. customwere purified by flash chromatography with hexane-ethyl acetate