反应详情

温度

0 °C

100 mg (0.27 mmol) thiazole-5-carboxylic acid (2-(4-iodophenyl)-1-methylethyl)-amide (I76) are added to 2.0 mL THF and cooled down to 0° C. 2.87 mg (4.00 μmol) bis(triphenylphosphine)palladium dichloride, 1.02 mg (5.00 μmol) CuI, 90.6 μL (0.65 mmol) diisopropylamine and finally 51.5 mg 2-cyclobutoxy-5-ethynyl-pyrimidine (I25.7) are added and the reaction mixture is stirred at r.t. over night. The solvent is removed in vacuo and the residue is dissolved in EtOAc and washed with diluted ammonia solution (1×) and water (2×). The organic layer is dried with MgSO4 and the solvent is removed in vacuo. The crude product is purified by HPLC (MeOH/H2O/TFA).

1. customThe solvent is removed in vacuo
2. dissolutionthe residue is dissolved in EtOAc
3. washwashed with diluted ammonia solution (1×) and water (2×)
4. dry with materialThe organic layer is dried with MgSO4
5. customthe solvent is removed in vacuo
6. customThe crude product is purified by HPLC (MeOH/H2O/TFA)