4-(2-Methylpiperidin-1-yl)-3-nitrobenzoic acid → 3-Amino-4-(2-methylpiperidin-1-yl)benzoic acid

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A methanolic solution of 4-(2-methylpiperidin-1-yl)-3-nitrobenzoic acid obtained in step 1 (500 mg; 1.89 mmol; 0.01 M) was pumped through an H-Cube (1 mL/min) fitted with a 10 mol % Pd/C catalyst cartridge (30×4 mm) and heated to 25° C. with the full hydrogen option enabled. Solvent was evaporated under vacuum to give the title compound as a pinkish oil (443 mg, 99%). 1H NMR (DMSO-d6, 300 MHz) δ 12.39 (bs, 1H), 7.28 (d, J=1.86 Hz, 1H), 7.14 (dd, J=8.1, 2.1 Hz, 1H), 6.99 (d, J=8.1 Hz, 1H), 5.01 (bs, 1H), 3.07-3.03 (m, 1H), 2.91-2.88 (m, 1H), 2.43-2.35 (m, 1H), 1.79-1.70 (m, 2H), 1.62-1.61 (m, 2H), 1.41-1.31 (m, 2H), 0.79 (d, J=6 Hz, 3H). HPLC (Method A) Rt 1.66 min (Purity: 99.2%).

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