Some tips on 3209-71-0

3209-71-0, 3209-71-0 Isoxazole-3-carboxylic Acid 11286453, aIsoxazoles compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3209-71-0,Isoxazole-3-carboxylic Acid,as a common compound, the synthetic route is as follows.

Amine 32-1 (73 mg, 0.209 mmol) was added to anhydrous dimethylformamide (2.0 mL). Isoxazole-3-carboxylic acid (23.6 mg, 0.209 mmol), EDC (40.1 mg, 0.209 mmol), HOBT (32 mg, 0.209 mmol) and triethylamine (58 0.418 mmol) were added sequentially and the resulting reaction mixture was allowed to stir at room temperature for 18 h. Following this duration, the contents were filtered and the resulting filtrate was purified via reverse-phase HPLC (5-95%, 0.1% TFA in H20:acetonitrile) to give 32-2 as a white solid. MS m/z (M+H): calculated = 445.1794; observed = 445.1808. NMR delta (ppm)(CHCl3-d): 8.50-8.43 (1 H, m), 7.14 (1 H, d, J = 8.42 Hz), 6.79-6.75 (1 H, m), 6.03 (1 H, d, J = 8.47 Hz), 5.10-5.01 (2 H, m), 4.18-4.08 (2 H, m), 3.90 (1 H, dd, J = 13.05, 3.18 Hz), 3.83-3.66 (3 H, m), 3.58-3.50 (1 H, m), 3.41 (3 H, d, J = 10.20 Hz), 2.15 (2 H, t, J = 14.76 Hz), 1.96 (4 H, d, J = 20.07 Hz).

3209-71-0, 3209-71-0 Isoxazole-3-carboxylic Acid 11286453, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; LAYTON, Mark, E.; PERO, Joseph, E.; RODZINAK, Kevin, J.; ROSSI, Michael, A.; WO2011/34741; (2011); A1;,
Isoxazole – Wikipedia
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