In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 202982-68-1 as follows. Recommanded Product: 202982-68-1
Example 131. Preparation of (4-(2-chloro-5-fluorophenyl)piperazin-1-yl)(5-phenylisoxazol-3-yl)methanone (297) To a solution of (5-phenylisoxazol-3-yl)(piperazin-1-yl)methanone (0.25 g, 0.851 mmol) and 1-chloro-4-fluoro-2-iodobenzene (0.327 g, 1.28 mmol) in toluene (5 mL) was added cesium carbonate (0.832 g, 2.55 mmol), tris(dibenzylideneacetone)dipalladium(0) (0.078 g, 0.085 mmol) and BINAP (0.053 g, 0.085 mmol). The reaction mixture was purged with nitrogen for 3 min and stirred at 115 C. in a sealed tube for 15 h. The mixture was quenched with water (10 mL) and extracted with ethyl acetate (15 mL*3). The combined organic layers were washed with brine (5 mL), dried over sodium sulfate, filtered and concentrated in vacuo. The crude product was purified by column chromatography (ISCO, 10 g silica, 8-10% ethyl acetate in petroleum ether, gradient over 15 min) and then by prep-HPLC (YMC-Actus ODS-AQ 100*30 5 mum column; 45-85% acetonitrile in an a 0.05% hydrochloric acid solution in water, 12 min gradient) to give (4-(2-chloro-5-fluorophenyl)piperazin-1-yl)(5-phenylisoxazol-3-yl)methanone hydrochloride salt (0.172 g, 0.404 mmol, 47%) as a white solid. 1H NMR (400 MHz, Chloroform-d) delta 7.89-7.80 (m, 2H), 7.57-7.46 (m, 3H), 7.40-7.31 (m, 1H), 6.89 (s, 1H), 6.82-6.71 (m, 2H), 4.20-4.10 (m, 2H), 4.08-3.97 (m, 2H), 3.18-3.13 (m, 4H); LCMS (ESI) m/z: 386.0 [M+H]+.
According to the analysis of related databases, 202982-68-1, the application of this compound in the production field has become more and more popular.
Reference:
Patent; Yumanity Therapeutics, Inc.; WRONA, Iwona; TIVITMAHAISOON, Parcharee; TARDIFF, Daniel; PANDYA, Bhaumik; OZBOYA, Kerem; LUCAS, Matthew; BOURDONNEC, Bertrand Le; (259 pag.)US2019/330198; (2019); A1;,
Iodide – Wikipedia,
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