Reference of 1458-01-1,Some common heterocyclic compound, 1458-01-1, name is Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate, molecular formula is C6H7ClN4O2, 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.
Preparation Example AA-1. 3,5-Diamino-pyrazine-2-carboxylic acid methyl ester To a solution of 3,5-diamino-6-chloro-pyrazine-2-carboxylic acid methyl ester (8.00g, 39.5mmol) in tetrahydrofuran (150mL) were added tetrakis(triphenylphosphine)palladium(0) (2.28g, 1.98mmol), formic acid (2.24mL, 59.3mmol) and triethylamine (16.5mL, 119mmol) at 0¡ãC under nitrogen atmosphere, then, the solution was stirred at 125¡ãC for 12 hours. The reaction solution was cooled to room temperature, and a solid precipitated. This solid was collected by filtration, and the title compound (10.7g, quantitatively) was obtained as a crude product of a white solid. 1H-NMR Spectrum (DMSO-d6) delta (ppm) : 3.70(3H, s), 6.95(2H, brs), 7.21 (1H, s).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate, its application will become more common.
Reference:
Patent; Eisai R&D Management Co., Ltd.; EP1782811; (2007); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem