HCID 53234295, compound → HCID 67173922, compound

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Reaction Steps

A solution of ethyl 3-(2-(N-(1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)sulfamoyl)-5-(2,2,2-trifluoroacetamido)phenyl)propanoate (50 mg, 0.1 mmol) in 7M ammonium in MeOH (10 mL) was stirred in a sealed tube at 50° C. for 6 hours. After concentrated, the crude mixture was purified by prep HPLC (SunFire Prep C18 OBD 5 uM 30×50 mm column) to give ethyl 3-(5-amino-2-(N-(1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)sulfamoyl)phenyl)propanoate as a white solid (22 mg, yield 54%) and methyl 3-(5-amino-2-(N-(1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)sulfamoyl)phenyl)propanoate as a white solid (7.3 mg, 19%).

Provenance & Evidence