Synthetic Route of 38487-86-4, These common heterocyclic compound, 38487-86-4, name is 2-Amino-4-chlorobenzonitrile, 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.
[00716] To a solution of compound 239-1 (1.3 g, 8.5 mmol, 1.0 eq) and [4-(trifluoromethyl)phenyl]boronic acid (2.43 g, 12.8 mmol, 1.5 eq) in DCM (20 mL) was added DIPEA (2.20 g, 17 mmol, 3 mL, 2.0 eq) and Cu(OAc)2 (2.32 g, 12.78 mmol, 1.5 eq) under N2. The suspension was degassed under vacuum and purged with 02 several times. The mixture was stirred under 02 (15 psi) at 25 C for 18 hours. TLC (Petroleum ether/ethyl acetate = 5/1, UV) indicated that the staring material was remained and two new spots were formed. LCMS showed that 16% of desired mass was detected. The reaction mixture was filtered and the filter was concentrated in vacuum. The residue was purified by column chromatography (Si02). Compound 239-2 (330 mg, 1.1 1 mmol, 13% yield) was obtained. 1HNMR (400 MHz, CDC13) 7.64 (d, J = 8.52 Hz, 2H), 7.49 (d, J= 8.52 Hz, 1H), 7.26 – 7.29 (m, 3H), 6.94 (dd, J = 8.42, 1.88 Hz, 1H), 6.55 (s, 1H).
Statistics shows that 2-Amino-4-chlorobenzonitrile is playing an increasingly important role. we look forward to future research findings about 38487-86-4.
Reference:
Patent; VIVACE THERAPEUTICS, INC.; KONRADI, Andrei W.; LIN, Tracy Tzu-Ling Tang; (396 pag.)WO2018/204532; (2018); A1;,
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