Reference of 847729-27-5 ,Some common heterocyclic compound, 847729-27-5, molecular formula is C7H5ClFNO2, 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.
Description 90: methyl 5-fluoro-2-(3-((4-fluoro-2- methylphenyl)amino)azetidin-1-yl)nicotinate (D90)A mixture of methyl 2-chloro-5-fluoronicotinate (D69) (199.85 mg, 1 .054 mmol) and potassium carbonate (291 mg, 2.108 mmol) in tetrahydrofuran (2ml) was stirred under N2 nitrogen 15 min at room temperature. N-(4-fluoro-2- methylphenyl)azetidin-3-amine (D55) (190 mg, 1 .054 mmol) was added and the resulting mixture was stirred 1 day at room temperature. The residue obtained after solvent evaporation was purified by Biotage SNAP-Si column eluting with a mixture cyclohexane/ethyl acetate from 100/0 to 80/20. Collected fractions after solvent evaporation afforded the title compound (D90)(155 mg)MS: (ES/+) m/z: 334.6 [MH+] C17H17F2N302 requires 333.331 H NMR (400MHz ,CHLOROFORM-d) delta = 8.24 (d, J = 2.9 Hz, 1 H), 7.80 (dd, J = 2.9, 8.3 Hz, 1 H), 6.91 – 6.75 (m, 2 H), 6.32 (dd, J = 4.9, 8.3 Hz, 1 H), 4.50 (dd, J = 7.3, 9.3 Hz, 2 H), 4.40 – 4.27 (m, 1 H), 3.97 – 3.81 (m, 5 H), 3.72 (d, J = 6.4 Hz, 1 H), 2.18 (s, 3 H)
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,847729-27-5, its application will become more common.
Reference:
Patent; ROTTAPHARM S.P.A.; BORRIELLO, Manuela; ROVATI, Lucio; STASI, Luigi Piero; BUZZI, Benedetta; COLACE, Fabrizio; WO2012/76063; (2012); A1;,
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