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. 1072-52-2, name is 2-(Aziridin-1-yl)ethanol. This compound has unique chemical properties. The synthetic route is as follows. Safety of 2-(Aziridin-1-yl)ethanol
Example 45(4-chlorophenyl)[4-chloro-3-phenyl-2-(2,2,2-trifluoroethoxy)quinolin-6-yl](1-methyl-1H-imidazol-5-yl)methanol TFA(100 mg, 0.202 rnniol, Example 65), 2,2,2 -trifluoroethanol (14,5 L, 0.202 mmol), toluene (2 ml), and sodium hydride (60% dispersion in mineral oil, 20 mg, 0.51 mmol) were combined in a round bottom flask under an N2atmosphere. The reaction solution was heated to reflux and reflux ed overnight. The reaction solution was cooled to room temperature then transferred to a separatory tunnel with EtOAc dilution, and extracted with saturated, aqueous NH4CI then saturated, aqueous NaHCOi solutions. The organic phase was separated then dried over MgS04, filtered and concentrated under reduced pressure. The crude product was purified by flash column chromatography (silica gel, 0-10% DCM / MeOH) then via reverse phase chromatography using acetonitrile with 0.05%) trifluoroacetic acid in water as eluent. The fractions from the purification containing the desired product were transferred to a separatory funnel with EtOAc and extracted with a saturated, aqueous NaHC03solution. The aqueous layer was separated, extracted with EtOAc, then the combined organic phases were dried over Mg804, filtered and concentrated under reduced pressure to provide the title compound. MS (ESS): mass caicd. for C28H20CI2F3N3O2, 557.1 ; m/z found, 558.3 [M+Hf; NMR (600 MHz, CDCI3) delta ppm 8.38 (s, 1 H), 8.17 (d, J = 2.0 Hz, 1H), 7.87 (d, J —— 8.8 Hz, 1H), 7.60 (dd, J —— 8.8, 2.1 Hz,1 1 1). 7.52 – 7.43 (m, 3H), 7.38 – 7.31 (m, 6H), 6.56 (s, 1 H), 4.92 (q, J —– 8.4 Hz, 21 1). 3.62 (s.
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Reference:
Patent; JANSSEN PHARMACEUTICA NV; BARBAY, Kent; EDWARDS, James, P.; KREUTTER, Kevin, D.; KUMMER, David, A.; MAHAROOF, Umar; NISHIMURA, Rachel; URBANSKI, Maud; VENKATESAN, Hariharan; WANG, Aihua; WOLIN, Ronald, L.; WOODS, Craig, R.; FOURIE, Anne; XUE, Xiaohua; CUMMINGS, Maxwell, D.; LEONARD, Kristi, A.; WO2015/57203; (2015); A1;,
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