Application of 7251-09-4, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 7251-09-4 as follows.
Step 1: Synthesis of 4-((4-amino-8-bromoquinazolin-2-yI)amino)-2-methoxybenzonitrile hydrochloride (Compound 3a) Compound 3a [0255] A mixture of 8-bromo-2-chloroquinazolin-4-amine (259 mg, 1 mmol, Ark Pharm Inc, AK-28702) and 4-amino-2-methoxybenzonitrile (222 mg, 1.5 mmol, Ark Pharm Inc, AK-77827) in isopropanol (7 mL) was heated in microwave at 180 C for 8 hours. The reaction mixture was cooled down to room temperature and the solid product was filtered off and washed with cold isopropanol and then with diethyl ether and hexane to afford the compound 3a as the HC1 salt. NMR (400 MHz, DMSO- /6) delta 8.24 (d, J = 8.1 Hz, 1H), 8.07 (d, J= 7.6 Hz, 1H), 7.59 (d, J= 8.5 Hz, 1H), 7.42 (dd, J = 8.6, 1.9 Hz, 1H), 7.37 – 7.04 (m, 5H), 3.99 (s, 3H). LCMS (m/z) 370.3 [M+H], Tr = 2.43 min (LCMS method 2).
According to the analysis of related databases, 7251-09-4, the application of this compound in the production field has become more and more popular.
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;,
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