反应详情

温度

100 °C

To a suspension of [4-(7-chloro-imidazo[1,2-a]pyridin-3-yl)-thiazol-2-ylmethyl]-carbamic acid tert-butyl ester (0.180 g, 0.49 mmol, 1.0 eq.) in dioxane/water (2:1, 6 mL), add 4-(methylsulphonyl)-benzeneboronic acid (0.108 g, 1.1 eq.), K3PO4 (0.208 g, 2.0 eq.), S-phos (0.025 g, 12.5% eq.) and Pd(OAc)2 (0.006 g, 0.05 eq.). Deoxygenate the reaction mixture and fill with nitrogen and stir at 100° C. for 4 hours. Cool the mixture to room temperature and dilute with 5:95 MeOH/DCM (100 mL). Wash the mixture with saturated aqueous saturated sodium chloride (2×20 mL), water (2×20 mL), dry, filter, and concentrate. Purify the residue on silica gel with a 0-80% EtOAc/Hexane gradient, then with 5:95 MeOH/DCM to give 0.160 g of the title compound as a slightly yellow solid.

1. customDeoxygenate the reaction mixture and fill with nitrogen
2. temperatureCool the mixture to room temperature
3. additiondilute with 5:95 MeOH/DCM (100 mL)
4. washWash the mixture with saturated aqueous saturated sodium chloride (2×20 mL), water (2×20 mL)
5. customdry
6. filtrationfilter
7. concentrationconcentrate
8. customPurify the residue on silica gel with a 0-80% EtOAc/Hexane gradient