Application of 33034-67-2, 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 33034-67-2 as follows.
Step 11: A mixture of (R)-methyl l-isopropyl-7-(methylsulfonyl)-l,2,3,4- tetrahydrobenzo[4,5]imidazo[l,2-a]pyrazine-8-carboxylate (0.9 g, 2.56 mmol), 2-chloro-4- (trifluoromethyl)pyrimidine (1.0 g, 5.1 mmol, 2 eq.) and DIEA (1.0 g, 7.7 mmol, 3 eq.) in i- PrOH (6 mL) was stirred in a microvave oven at 150 °C for 2 h. TLC showed the starting material was consumed completely (PE : EtOAc = 3 : 1). The solvent was removed in vacuo at 40 °C, and the residue was purified by column chromatography on silica gel eluting with PE / EtOAc = 6 / 1 to give (R)-methyl l-isopropyl-7-(methylsulfonyl)-2-(4- (trifluoromethyl)pyrimidin-2-yl)-l,2,3,4-tetrahydrobenzo[4,5]imidazo[l,2-a]pyrazine-8- carboxylate (1.0 g, 78percent yield) as a white solid.LC-MS m/z 498.1 [M+H]+. 1H NMR (CDC13 300MHz): delta 8.52 (d, 7 = 4.8 Hz, 1H), 8.13 (s, 1H), 8.06 (s, 1H), 6.83 (d, 7 = 4.8 Hz, 1H), 6.06 (d, 7 = 7.8 Etazeta,IotaEta), 5.39-5.28 (m, 1H), 4.33-4.24 (m, 1H), 4.20-4.12 (m, 1H), 3.93 (s, 3H), 3.77-3.65 (m, 1H), 3.39 (s, 3H), 2.52-2.38 (m, 1H), 1.25 (d, 7 = 6.9 Hz, 3H), 1.02 (d, 7 = 6.6 Hz, 3H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,33034-67-2, its application will become more common.
Reference:
Patent; VITAE PHARMACEUTICALS, INC.; DONG, Chengguo; FAN, Yi; LEFTHERIS, Katerina; LOTESTA, Stephen; SINGH, Suresh, B.; TICE, Colin; ZHAO, Wei; ZHENG, Yajun; ZHUANG, Linghang; WO2013/138565; (2013); A1;,
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