Application of 4949-13-7,Some common heterocyclic compound, 4949-13-7, name is 2-Fluoropyrazine, molecular formula is C4H3FN2, 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.
[0222] To a mixture of (A)-4-( l -aminocthyljhcnzonitrilc (1.0 g, 6.8 mmol, 1.0 equiv) and IPA (15 mL) in a microwave vial (20 mL) were added 2-fluoropyrazine (0.81 g, 8.2 mmol, 1.2 equiv) and DIPEA (2.1 g, 16.4 mmol, 2.4 equiv). The vial was sealed and heated at 170 C in a microwave reactor for 4 h. The mixture was concentrated onto 5 g of Si02 and purified by silica gel chromatography (40 g column, 0-10% MeOH in DCM) to provide (/?)- 4-(l-(pyrazin-2-ylamino)ethyl)benzonitrile. LRMS (ES) m/z 225.1 (M+H). 1 H-NMR (Methanol-74, 400 MHz, ppm) d 7.92 (t, J = 1.7 Hz, 1H), 7.85 (dd, 7 = 2.9, 1.5 Hz, 1H), 7.70 – 7.63 (m, 2H), 7.61 (d, 7 = 2.9 Hz, 1H), 7.58 – 7.52 (m, 2H), 5.08 (q, 7 = 7.1 Hz, 1H), 1.54 (d, 7 = 7.0 Hz, 3H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Fluoropyrazine, its application will become more common.
Reference:
Patent; CYTOKINETICS, INC.; MORGAN, Bradley P.; VANDERWAL, Mark; CHUANG, Chihyuan; (0 pag.)WO2020/5888; (2020); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem