Electric Literature of 153800-11-4, These common heterocyclic compound, 153800-11-4, name is 2-Ethynylpyrazine, 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 231(100mg, 0.282mmo1) and 10(58.8mg, 0.565mmo1) in 2OmL of Et3N was added Pd(PPh3)2C12 (991mg, 0Oi4mmol) and Cul (538mg, 0O28mmol). The mixture was protected with N2 atmosphere, then was heated at 70C for 4 hours. TLC analysis showedcomplete conversion of starting material to a major product. The reaction mixture was then concentrated in vacua The crude product was purified by Prep-HPLC to give the target product Compound 125(23mg, yield: 24.66%).LCMS: in/z 331 (M+HY?H NMR (400 MHz, CDCI3): d 8.83 (d, J:::: 6.4 Hz, 11:1), 862 (s, 11:1), 854 (s, 1H), 793 (d, J:::2.4 Hz, IH), 7.79-7.75 (m, 2H), 735-733 (m, 2H), 6.79 (d, J= 2.4 Hz, 1H).
The synthetic route of 153800-11-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; HUA MEDICINE (SHANGHAI) LTD.; CHEN, Li; JIN, Xiaowei; (176 pag.)WO2017/117708; (2017); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem