Application of 1236000-51-3, A common heterocyclic compound, 1236000-51-3, name is N-Methyl-1-(4-(trifluoromethoxy)phenyl)methanamine hydrochloride, molecular formula is C9H11ClF3NO, 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.
Intermediate 28 To a solution of 1.0 g of 3-iodobenzoic acid in 20 ml of CH2CI2 under argon atmosphere was added via cannula a solution of 1.11 g of DCC in 22 ml of CH2CI2. The resulting mixture was stirred for 1 h, then was added a solution of 0.65 g of Intermediate 1 and 0.414 ml of Et3N in 13 ml of CH2CI2. The resulting mixture was stirred overnight, diluted with Et2O, filtered off and the filter cake washed with Et2O. The filtrate was washed with 10% NaHCO3 and brine, dried over MgSO4, filtered and concentrated under vacuum. The residue was purified by chromatography on silica gel eluting with EtOAc-Hex 10:90 to 50:50 to afford 1.063 g (91 %) of the title compound as a colourless oil. 1H NMR (delta, ppm, CDCI3): 7.79 and 7.75 (s, 1 H); 7.39 (s, 1 H); 7.23 (d, 2H); 7.21-7.1 1 (m, 2H); 4.72 and 4.49 (s, 2H); 3.02 and 2.88 (s, 3H). [ES MS] m/z: 436 (MH+).
The synthetic route of 1236000-51-3 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GLAXO GROUP LIMITED; BUENO-CALDERON, Jose Maria; FERNANDEZ-MOLINA, Jorge; LEON-DIAZ, Maria Luisa; MALLO-RUBIO, Araceli; MANZANO-CHINCHON, M Pilar; WO2010/81904; (2010); A1;,
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