Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 1001413-01-9, name is 1-(3,4-Difluorobenzyl)-2-oxo-1,2-dihydropyridine-3-carboxylic acid. This compound has unique chemical properties. The synthetic route is as follows. HPLC of Formula: C13H9F2NO3
The carboxylic derivative 3 (300 mg, 1.13 mmcl) and the amine 2(168 mg, 1.13 mmcl) were combined through a condensation reaction in presence of thecondensing agent TBTU (363 mg, 1.13 mmol). The solvents were evaporated under reduced pressure and the crude product was purified by flash chromatography over silica gel, using 0 – 4% MeOH as a gradient in CHCI3, to obtain pure SST143 as a white solid (210 mg, 0.53 mmol, 47% yield). mp: 285-288 00 1H-NMR (400 MHz, DMSO-d6): 6 3.48 (5, 2H, CH2 indole); 5.28(5, 2H, CH2); 6.68 (dd, 1 H, J= 6.8, 7.2 Hz, Ar); 6.77 (d, 1 H, J= 8.4 Hz, Ar); 7.20-7.23 (m, 1H, Ar); 7.40-7.52 (m, 3H, Ar); 7.66 (5, 1H, Ar); 8.29 (dd, 1H, J= 2.2,6.8 Hz, Ar); 8.46 (dd, 1H, J= 2.2, 6.8 Hz, Ar); 10.33 (5, 1H, NH), 11.87 (5, 1H,NH) ppm. 13C-NMR (101 MHz, DMSO-d6): 6 176.23, 161.54, 160.73, 150.35,147.90, 143.78, 143.42, 139.86, 134.02, 132.32, 126.40, 124.90, 120.35,119.02, 117.74, 117.25, 116.90, 109.10, 107.22, 51.45, 36.02 ppm. 19F-NMR (376 MHz; DMSO-d6): 6-138.17 (d, iF, J= 24 Hz); -139.76 (d, iF, J= 24 Hz) ppm. Anal. Calcd for 021H15F2N303: 0, 63.80%; H, 3.82%; N 10.63%; Found: C, 63.72%; H, 3.55%; N, 10.50%
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Reference:
Patent; INTERNATIONAL SOCIETY FOR DRUG DEVELOPMENT S.R.L.; SESTITO, Simona; DANIELE, Simona; MARTINI, Claudia; RAPPOSELLI, Simona; PURICELLI, Guido; (63 pag.)WO2016/198597; (2016); A1;,
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