431-38-9 , The common heterocyclic compound, 431-38-9, name is 3-Amino-1,1,1-trifluoropropan-2-ol, molecular formula is C3H6F3NO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
A solution of 130mg intermediate ii, 101 mg 3-amino-1,1,1-trifluoropropan-2-ol, 224mg HATU and 0.21 mL ethyldiisopropylamine in 10 mL of DMF was stirred at room temperature for 14 hours. Then the reaction was quenched by water, and the mixture was extracted with dichloromethane two times. The combined organic phases were dried over sodium sulfate and evaporated to dryness. The residue was subjected to flash chromatography (dichloromethanemethanol gradient with up to 2% methanol) to yield 160 mg 6-(4-chlorophenyl)-2-(1 -methyl-i,3,3-trifluoro-2-hydroxypropyl)-2 ,3-di hydropyridazi ne-4-carboxamide.1H-NMR (400 MHz, CDCI3): 6 [ppm] = 3.70-3.79 (m, 1H); 3.93 (ddd, 1H); 3.98 (s, 3H); 4.21-4.28 (m, 1 H); 4.64 (br s, 1 H); 7.49 (d, 2H); 7.85 (d, 2H); 8.11 (s, 1 H); 8.31 (s, 1 H); 8.66 (s, 1i0.15(bt,1H).
According to the analysis of related databases, 431-38-9, the application of this compound in the production field has become more and more popular.
Reference:
Patent; BAYER AKTIENGESELLSCHAFT; BAYER PHARMA AKTIENGESELLSCHAFT; DEUTSCHES KREBSFORSCHUNGSZENTRUM; GUTCHER, Ilona; ROeHN, Ulrike; SCHMEES, Norbert; ZORN, Ludwig; ROeSE, Lars; BADER, Benjamin; KOBER, Christina; CARRETERO, Rafael; STOeCKIGT, Detlef; IRLBACHER, Horst; PLATTEN, Michael; (397 pag.)WO2018/146010; (2018); A1;,
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