1083224-23-0, 5-(2,4-Difluorophenyl)isoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated
General procedure: To a solution of (3S,4S)-4-amino-piperidine-1 ,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester (1 g, 3.87 mmol) in DMF (8 mL) at RT is added 5-(2,4-difluorophenyl)isoxazole-3- carboxylic acid (1.3 g, 5.81 mmol). DIPEA (2.12 mL, 12.4 mmol) is then added followed by HATU (1.55 g, 4.06 mmol). The reaction mixture is stirred overnight at RT. The reaction mixture is concentrated, dissolved in DCM (100 mL) and treated twice with aq. sat. NaHC03 (l OOmL). The organic layer is dried over MgS04 and evaporated. The crude residue is purified by flash chromatography over 40 g of silica gel with heptane/EtOAc system (1 :0 to 3:1 )as eluent to yield the title compound as white powder; LC-MS method A: tR = 0.94 min; [M+H]+ = 466.04. 1H NMR (400 MHz, CDCI3) <5: 7.23-7.36 (m, 1 H), 7.96 (m, 1 H), 6.96-7.12 (m, 3 H), 6.79-6.91 (m, 1 H), 4.29-4.51 (m, 2 H), 4.00-4.22 (m, 1 H), 3.64-3.78 (m, 3 H), 2.85- 3.09 (m, 2 H), 2.50-2.68 (m, 1 H), 2.10-2.27 (m, 1 H), 1.42-1.69 (m, 1 1 H), 1.21-1.38 (m, 1 H). 1083224-23-0, 1083224-23-0 5-(2,4-Difluorophenyl)isoxazole-3-carboxylic acid 28951583, aIsoxazoles compound, is more and more widely used in various.
Reference£º
Patent; IDORSIA PHARMACEUTICALS LTD; AISSAOUI, Hamed; GUERRY, Philippe; LEHEMBRE, Francois; POTHIER, Julien; POUZOL, Laetitia; RICHARD-BILDSTEIN, Sylvia; YUAN, Shuguang; (273 pag.)WO2018/19929; (2018); A1;,
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