63874-95-3, name is 1-Benzyl-1H-pyrazole-4-carbaldehyde, belongs to pyrazoles-derivatives compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Recommanded Product: 63874-95-3
General procedure: Step 7. Preparation of (S)-5-chloro-4-((1-((6-(difluoromethyl)-3-fluoropyridin-2- yl)methyl)pyrrolidin-3-yl)(methyl)amino)-2-fluoro-//-(thiazol-4- yl)benzenesulfonamide formate To a solution of (S)-5-chloro-2-fluoro-4-(methyl(pyrrolidin-3-yl)amino)-//- (thiazol-4-yl)benzenesulfonamide (0.100 g, 0.234 mmol) and 6-(difluoromethyl)-3- fluoropicolinaldehyde (0.102 g, 0.585 mmol) in dichloromethane (5 ml_) was added acetic acid (0.50 ml_) and sodium triacetoxyborohydride (0.148 g, 0.702 mmol) portionwise and the resulting mixture was stirred at ambient temperature for 1 h. Concentration in vacuo and purification of the residue by preparative reverse phase HPLC, using acetonitrile in water containing 0.225% formic acid as eluent, afforded the title compound as a colorless solid (0.017 g, 13% yield): H NMR (400 MHz, CD3OD) delta 8.74 (d, J = 2.2 Hz, 1 H), 8.40 (br s, 0.8H), 7.83-7.71 (m, 3H), 7.04 (d, J = 2.2 Hz, 1 H), 7.00 (d, J = 12.0 Hz, 1 H), 6.75 (t, J = 55.2 Hz, 1 H), 4.35-4.26 (m, 1 H), 4.16-4.02 (m, 2H), 3.09-2.96 (m, 3H), 2.92-2.84 (m, 1 H), 2.83 (s, 3H), 2.22-2.12 (m, 1 H), 2.05-1.92 (m, 1 H), NH and COOH not observed; MS (ES+) m/z 549.9 (M + 1), 551.9 (M + 1).
The synthetic route of 63874-95-3 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; XENON PHARMACEUTICALS INC.; ANDREZ, Jean-Christophe; BURFORD, Kristen, Nicole; CHOWDHURY, Sultan; COHEN, Charles, Jay; DEHNHARDT, Christoph, Martin; DEVITA, Robert, Joseph; EMPFIELD, James, Roy; FOCKEN, Thilo; GRIMWOOD, Michael, Edward; HASAN, Syed, Abid; JOHNSON, James, Philip, Jr.; ZENOVA, Alla, Yurevna; (493 pag.)WO2017/201468; (2017); A1;,
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