Electric Literature of 153800-11-4,Some common heterocyclic compound, 153800-11-4, name is 2-Ethynylpyrazine, molecular formula is C6H4N2, 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 227(100mg, 0.3O6mrnoI) and 10(63.7mg, 0.61 immol) in 2OmL of Et3N was added Pd(PPh3)2C12 (10.73mg, 0.OiSmrnoi) and CuT (5.82mg, 0.03 immol). The mixture was protected with N2 atmosphere, then was heated at 70C for 24 hours. TLC analysis showed complete conversion of starting material to a major product. The reaction mixture was then concentrated in vacuo. The crude product was purified by Prep-IPLC to give the target productCompound 103(18mg, yield: 1941 %).LCMS: m/z 304 (M+H)NMR (400 MHz, CDCI3): 5 8.668.65 (m, 3H), 7.67 (s, 1H), 7.60-7.57 (m, IH), 7.43.-7.40 (m, 1H), 6.55 (s, 11:1), 2.47 (s, 31:1).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Ethynylpyrazine, its application will become more common.
Reference:
Patent; HUA MEDICINE (SHANGHAI) LTD.; CHEN, Li; JIN, Xiaowei; (176 pag.)WO2017/117708; (2017); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem