Electric Literature of 431-38-9, 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 431-38-9 as follows.
2-(3-Fluorophenyl)-3-oxo-6-[4-(trifluoromethyl)phenyl]-2,3-dihydropyridazine-4-carboxylic acid (100 mg, 0.26 mmol) was dissolved in anhydrous DMF (2 mL). (2RS)-3-Amino-1 ,1 ,1 – trifluoropropan-2-ol (68 mg, 0.53 mmol), N-ethyl-N-isopropylpropan-2-amine (0.207 mL, 1.19 mmol), and propane phosphonic acid anhydride (T3P, 231 muIota_, 50% in DMF, 397 muetaetaomicronIota) were successively added. It was stirred at rt overnight. The crude reaction mixture was purified by RP-HPLC (column: X-Bridge C18 5muetaiota 100x30mm, mobile phase: (water + 0.1 vol% formic acid (99%)) / acetonitril gradient) to yield 73.9 mg (57%) of the title compound. 1H-NMR (400MHz, DMSO-de): delta [ppm] = 3.48 (ddd, 1 H), 3.71 – 3.80 (m, 1 H), 4.17 – 4.29 (m, 1 H), 6.67 (d, 1 H), 7.37 – 7.44 (m, 1 H), 7.55 – 7.59 (m, 1 H), 7.60 – 7.67 (m, 2H), 7.89 (d, 2H), 8.20 (d, 2H), 8.74 (s, 1 H), 9.62 (t, 1 H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,431-38-9, its application will become more common.
Reference:
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; DEUTSCHES KREBSFORSCHUNGSZENTRUM (DKFZ); SCHMEES, Norbert; GUTCHER, Ilona; IRLBACHER, Horst; BADER, Benjamin; ZHAO, Na; PLATTEN, Michael; (437 pag.)WO2017/202816; (2017); A1;,
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