Reference of 4426-11-3, These common heterocyclic compound, 4426-11-3, name is Cyclobutanecarbonitrile, 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.
[00140] To a mixture of cyclobutanecarbonitrile (0.70 g, 8.6 mmol) and 2-chloro-6- fluorobenzoic acid (0.5 g, 2.9 mmol) in THF (9.6 mL) at 0 C was added KHMDS (0.5M in toluene, 12.6 mL, 6.3 mmol). The resulting mixture was heated at 70 C for 3h, then cooled down, concentrated in vacuo. The residue was taken up in 20mL H20, and extracted with Et^O for three times. The aqueous layer was acidified with 2N HC1, and extracted with CHCI3/1- PrOH (3: 1). The combined organics were dried over Na2SC>4, concentrated. The crude residue was used directly. MS: 236 (M+l). XH NMR (600 MHz, DMSO-d6): delta 12.9-13.1 (brs, 1H), 7.51 (dd, 1H, J= 8.4, 1.2Hz), 7.46 (t, lH, J= 8.4 Hz), 7.30 (dd, 1H, J= 8.4, 1.2 Hz), 2.56- 2.68(m, 4H), 2.22-2.32 (m, 1H), 1.84-1.90 (m, 1H).
The synthetic route of 4426-11-3 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MERCK SHARP & DOHME CORP.; LAPOINTE, Blair, T.; FULLER, Peter, H.; GUNAYDIN, Hakan; LIU, Kun; SCOTT, Mark, E.; TROTTER, B., Wesley; ZHANG, Hongjun; (211 pag.)WO2017/75182; (2017); A1;,
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