864293-44-7

General procedure for the synthesis of 2-amino-5-bromo-3-methoxybenzoic acid from 2-amino-3-methoxybenzoic acid: 2-amino-3-methoxybenzoic acid (10.0 g, 59.8 mmol, 1.0 eq.) was dissolved in dichloromethane (DCM, 150 mL), followed by addition of N-bromosuccinimide (NBS, 10.6 g, 59.8 mmol 1.0 eq.). The reaction mixture was stirred at room temperature for 2 hours. Upon completion of the reaction, the solid product was collected by filtration and washed with dichloromethane (100 mL x 2) to give the final 2-amino-5-bromo-3-methoxybenzoic acid as a gray solid (12.1 g, 82.2% yield).

[1] Patent: US2009/203657, 2009, A1. Location in patent: Page/Page column 50
[2] Patent: US2009/203677, 2009, A1. Location in patent: Page/Page column 53
[3] Patent: US2009/197871, 2009, A1. Location in patent: Page/Page column 52-53
[4] Patent: WO2009/100169, 2009, A1. Location in patent: Page/Page column 131
[5] Journal of Medicinal Chemistry, 2018, vol. 61, # 14, p. 6087 - 6109