Application of 167837-43-6 ,Some common heterocyclic compound, 167837-43-6, molecular formula is C8H8N2O2, 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 (E)-3-(6-aminopyridin-3-yl)acrylic acid (123 mg, 0.75 mmol) in DMF (4 mL) was added (lambda)-methyl-[l-(3-ethyl-benzofuran-2-yl)-ethyl]amine (183 mg, 0.90 mmol), EDCI (187 mg, 0.98 mmol), HOBt (112 mg, 0.83 mmol) and DIPEA (0.45 mL, 2.33 mmol). The mixture was stirred at 40 0C for 60 hours. The mixture was diluted with H2O (30 mL) and the solid collected by filtration. The solid was washed with 100 mL H2O and then dried under reduced pressure overnight. It was purified by chromatography (silica, 1.5% MeOH in CH2Cl2) to give 79 mg (25%) of title compound as a mixture of amide rotamers. 1H NMR (300 MHz, CDCl3, delta) 8.22 (s, IH), 7.7-7.1 (m, 6H), 6.8-6.2 (m, 3H), 4.72 (s, 2H) 3.06 (s, 3H), 2.74 (s, 2H), 1.9-1.1 (m, 6H); MS (ESI) m/e 350 (M + H)+.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,167837-43-6, its application will become more common.
Reference:
Patent; AFFINIUM PHARMACEUTICALS, INC.; WO2007/67416; (2007); A2;,
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