Electric Literature of 31108-57-3, These common heterocyclic compound, 31108-57-3, name is 1H-Pyrazole-4-carbonitrile, 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 II-F10 (49.4 mg, 0.1 mmol) and lH-pyrazole-4-carbonitrile (22.3 mg, 0.2 mmol) in acetone (2 mL) was added K2C03 (33.1 mg, 0.24 mmol). After stirring at 20 C for 16 h, the reaction mixture was extracted with EtOAc (3 x 30 mL). The combined organic solution was washed with saturated brine (30 mL), dried over anhydrous Na2S04, filtered and concentrated. The residue was purified by flash column (0-20% of EtOAc in PE) to give II- Fll (28.5 mg, 56%) as a solid. (2792) 1H NMR (400 MHz, CDCl3) dH 7.85 (s, 1H), 7.81 (s, 1H), 5.06-4.86 (dd, J= 17.6, 47.6 Hz, 2H) , 2.60 (t, j= 8.8 Hz), 2.27-2.15 (m, 1H), 2.06-1.99 (m, 1H), 1.84-1.67 (m, 6H), 1.56- 1.37 (m, 8H), 1.33-0.80 (m, 13H), 0.67 (s, 3H); LC-ELSD/MS purity 99.30%, MS ESI calcd. for C26H36N30[M-H20+H]+ 406.29, found 406.3.
The synthetic route of 31108-57-3 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; SAGE THERAPEUTICS, INC.; ROBICHAUD, Albert, Jean; SALITURO, Francesco, G.; BLANCO-PILLADO, Maria, Jesus; LA, Daniel; HARRISON, Boyd, L.; (646 pag.)WO2019/126761; (2019); A1;,
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