3-bromo-5-fluoro-2-hydroxybenzoic acid synthesis

Yield:4180-42-1 85%

Reaction Conditions:

with NBS;glacial acetic acid at 80; for 24 h;

Steps:

37.1 Synthesis of 37B

A mixture of 37A (5.1 g, 33 mmol, 1.0 eq) and NBS (6.4 g, 36 mmol, (0957) 1.1 eq) in AcOH (25 mL) was stirred at 80 °C for 24 hours. The reaction was monitored by TLC. The mixture was concentrated in vacuo and the residue was purified by column chromatography (PE/EA = 2: 1 to 1 : 1 ) to give 37B (6.5 g, 85%). ESI-MS: [M-H]^": 233,235

References:

WO2016/149393,2016,A1 Location in patent:Paragraph 0350