Application of 1788-08-5, These common heterocyclic compound, 1788-08-5, name is 4-Ethynylbenzenesulfonamide, 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.
To a solution of 4-ethynylbenzenesulfonamide (800 mg, 4.419 mmol, Intermediate 71 ) and 4- (azidomethyl)pyridine (583 mg, 4.417 mmol, Intermediate 55) in a mixture of ethanol (10 mL) and water (10 mL), copper sulphate pentahydrate (1 10 mg, 0.442 mmol) and sodium-L-ascorbate (262 mg, 1.323 mmol) were added at 26 C and stirred at 26 C for 16 h. Upon completion, the reaction mixture was concentrated under reduced pressure. The crude was purified by column chromatography (silicagel 100-200 mesh), eluted with 10% methanol in dichloromethane. The pure fractions were collected and concentrated under reduced pressure to afford 4-(1 -(pyridin-4- ylmethyl)-1 H-1 ,2,3-triazol-4-yl)benzenesulfonamide (500 mg, crude) as a brown solid.1H NMR (400 MHz, DMSO-de) delta 8.81 (s, 1 H), 8.65-8.55 (m, 2H), 8.05 (d, J = 8.4 Hz, 2H), 7.89 (d, J = 8.4 Hz, 2H), 7.48 – 7.22 (m, 4H), 5.76 (d, J = 6.7 Hz, 2H). MS m/z [M+H]+= 316.15.
Statistics shows that 4-Ethynylbenzenesulfonamide is playing an increasingly important role. we look forward to future research findings about 1788-08-5.
Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; ALEMPARTE-GALLARDO, Carlos; ENCINAS, Lourdes; ESQUIVIAS PROVENCIO, Jorge; (206 pag.)WO2019/34729; (2019); A1;,
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