Reference of 113305-94-5, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 113305-94-5, name is 5-Aminopyrazine-2-carbonitrile belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below.
EXAMPLE 26 (E)-5-((4-Amino-8-(4-(2-cyanovinyl)-2,6-dimethylphenyI)-6-fluoroquinazoIin-2- yl)amino)pyrazine-2-carbonitrile- Compound 26 Synthesis of (E)-5-((4-amino-8-(4-(2-cyanovinyl)-2,6-dimethylphenyl)-6- fluoroquinazoIin-2-yl)amino)pyrazine-2-carbonitrile (compound 26) Compound 26 [0314] Compound 20d (92 mg, 0.21 mmol), 5-aminopyrazine-2-carbonitrile (60 mg, 0.50 mmol, Ark Pharm Inc, AK-21935), N,N-diisopropylethylamine (174 1 .0 mmol), (9,9- dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (24 mg, 0.042 mmol) and palladium (II) acetate (9 mg, 0.042 mmol) were combined under argon in N-methyl-2-pyrrolidone (2 mL). The reaction was heated at 100C in a sealed vessel for 7 hours. The reaction mixture was cooled down to room temperature, purified by silica gel chromatography (gradient from 50- 100% ethyl acetate in wo-hexanes) and then re-purified by reverse phase chromatography (5- 100% acetonitrile in water with 0.1 % trifluoroacetic acid) to afford the TFA salt of compound 26. ‘H NMR (400 MHz, DMSO-flfc) delta 9.10 (s, 1 H), 8.20 (s, 1 H), 7.74 (d, J = 16.7 Hz, 1 H), 7.77 – 7.60 (m, 2H), 7.57 (s, 2H), 6.56 (d, J = 16.7 Hz, 1 H), 1.94 (s, 6H). LCMS (m/z) 436.9 [M+H], Tr = 3.59 min (LCMS method 1 ).
The synthetic route of 5-Aminopyrazine-2-carbonitrile has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GILEAD SCIENCES, INC.; INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY OF THE AS CR, V.V.I.; JANSA, Petr; SIMON, Tetr; LANSDON, Eric; HU, Yunfeng, Eric; BASZCZYNSKI, Ondrejj; DEJMEK, Milan; MACKMAN, Richard, L.; (185 pag.)WO2016/105564; (2016); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem