Electric Literature of 13484-56-5, These common heterocyclic compound, 13484-56-5, name is 3-Chloro-6-methoxypyrazin-2-amine, 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.
Sodium hexamethyldisilazane (1M solution in THF; 6.7 ml) was added dropwise to amixture of 3-amino-2-chloro-5-methoxypyrazine (0.64 g), 4-chloro-7-(2-chloroethoxy)-3-cyano-6-methoxyquinoline (J. Med. Chem., 2001,44, 3965-3977; 1 g) andDMF (10 ml) thathad been cooled to 0C. The mixture was stirred at 0C for 5 minutes and at ambienttemperature for 30 minutes. Acetic acid (0.38 ml) was added and the resultant mixture wasevaporated. The residue was partitioned between methylene chloride and a 5% aqueoussodium bicarbonate solution. The organic solution was dried over magnesium sulphate andevaporated. The residue was triturated under diethyl ether and the resultant solid was isolated.There was thus obtained the title compound as a solid (0.98 g); Mass Spectrum: M+H1″ 420and 422.
The synthetic route of 13484-56-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/108703; (2004); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem