The origin of a common compound about 875781-43-4

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference of 875781-43-4, A common heterocyclic compound, 875781-43-4, name is 2-Bromo-5H-pyrrolo[2,3-b]pyrazine, molecular formula is C6H4BrN3, 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.

2-Bromo-5H-pyrrolo [2,3-b] pyrazine (300 mg, 1.52 mmol) was dissolved in N, N- dimethylformamide (8 mL)Sodium hydride (60%, 91.3 mg, 2.28 mmol) was added under ice bath and stirring continued at this temperature. After 30 min 2- (trimethylsilyl) ethoxymethyl chloride (404 muL, 2.26 mmol ),Stir at room temperature for 12h. Quenched with water (20 mL)The mixture was extracted with dichloromethane (30 mL × 2) and concentrated for column chromatography (eluent: PE / EtOAc (v / v) = 5/1) to give 270 mg of a yellow oil. Yield: 54.3%.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Liu Bing; Bai Shun; Zhou Youbo; Yang Tiping; He Wei; Zhang Yingjun; Zheng Changchun; (103 pag.)CN106749268; (2017); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem