反应详情

温度

130 °C

To a 20 mL microwave vial was added N-cyclopropyl-5-(3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1-tosyl-1H-indol-5-yl)-1,3,4-oxadiazol-2-amine (200 mg, 0.456 mmol), 2-chloro-6-cyclopropylpyrazine (CombiPhos Catalysts Inc., 78 mg, 0.502 mmol), dicyclohexyl(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphine (13.05 mg, 0.027 mmol), Pd2(dba)3 (12.5 mg, 0.014 mmol), and potassium phosphate (291 mg, 1.369 mmol) followed by purging with argon. The solids were treated with dioxane (4.0 mL) and water (0.4 mL) and heated in the microwave at 130° C. for 20 min. The mixture was treated with H2O and extracted with EtOAc, dried over MgSO4, filtered and concentrated. Purification (0-100% EtOAc in Hex) afforded N-cyclopropyl-5-(3-(6-cyclopropylpyrazin-2-yl)-1-tosyl-1H-indol-5-yl)-1,3,4-oxadiazol-2-amine (45.6 mg, 19%) as a pale yellow solid. MS (ESI, pos. ion) m/z: 513.1 (M+1).

1. customby purging with argon
2. additionThe solids were treated with dioxane (4.0 mL) and water (0.4 mL)
3. additionThe mixture was treated with H2O
4. extractionextracted with EtOAc
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. concentrationconcentrated
8. customPurification (0-100% EtOAc in Hex)