Reference of 1458-18-0, A common heterocyclic compound, 1458-18-0, name is Methyl 3-amino-5,6-dichloropyrazine-2-carboxylate, molecular formula is C6H5Cl2N3O2, 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.
The mixture of methyl 3-amino-5, 6-dichloropyrazine-2-carboxylate (0.5 g, 2.26 nMol) , (1-methyl-1H-pyrazol-4-yl) boronic acid (0.43 g, 3.39 nMol) in dioxane (20 mL) was added Na 2CO 3 (0.57 g, 4.53 nMol) and Pd (dppf) Cl 2 (0.83 g, 1.13 nMol) at 100 . Then the mixture was stirred at this temperature for 2h. LCMS showed the reaction was completed and purified with silica gel chromatography to give a desired product methyl 3-amino-6-chloro-5- (1-methyl-1H-pyrazol-4-yl) pyrazine-2-carboxylate. LCMS: m/z (ESI) , [M+H] + = 268.6.
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; DIZAL (JIANGSU) PHARMACEUTICAL CO., LTD.; QI, Changhe; TSUI, Honchung; ZENG, Qingbei; YANG, Zhenfan; ZHANG, Xiaolin; (399 pag.)WO2020/35052; (2020); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem