反应详情

A solution of boronic acid 11 (700 mg, 1.72 mmol) in DCM (15 mL) at 0° C. is treated with triethylamine (0.48 mL, 3.45 mmol), followed by 3-chlorobenzo-[b]thiophene-2-carbonyl chloride (439 mg, 1.90 mmol) in one portion. After warming to RT, the solution is stirred 16 h. Analysis by LC/MS at this juncture confirmed the reaction is complete. Thus the reaction is diluted with aqueous NaHCO3 (20 mL) and extracted into EtOAc (3×25 mL). The combined EtOAc phases are dried (Na2SO4) and reduced in vacuo to afford the title compound.

1. extractionextracted into EtOAc (3×25 mL)
2. dry with materialThe combined EtOAc phases are dried (Na2SO4)