反应详情

温度

100 °C

[4-(4-Isopropyl-phenyl)-thiazol-2-yl]-thiophen-2-ylmethyl-amine (50 mg, 0.16 mmol), 4-(chlorosulfonyl)benzoic acid (53 mg, 0.24 mmol), triethylamine (45 μL, 0.32 mmol), and DMAP (2 mg, 0.016 mmol) were combined in DCM (2 mL). The resulting reaction mixture was heated in a CEM Exployer PLS™ microwave at 100° C. for 30 min. After cooling to room temperature, saturated NaHCO3 (aq) solution (5 mL) was added. The mixture was extracted with DCM (2×4 mL). The combined organic layer was dried over Na2SO4 and concentrated. Purification of the crude product was carried out using silica gel chromatography eluting with DCM/MeOH 9:1, yielding 4-{[4-(4-isopropyl-phenyl)thiazol-2-yl]-thiophen-2-ylmethyl-sulfamoyl}-benzoic acid. LCMS m/z: 500 (M+1)+.

1. customThe resulting reaction mixture
2. temperatureAfter cooling to room temperature
3. extractionThe mixture was extracted with DCM (2×4 mL)
4. dry with materialThe combined organic layer was dried over Na2SO4
5. concentrationconcentrated
6. customPurification of the crude product
7. washeluting with DCM/MeOH 9:1