Reference of 187035-79-6, 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 187035-79-6 as follows.
To a solution of (R)-methyl l-isopropyl-7-(methylsulfonyl)-l,2,3,4- tetrahydrobenzo[4,5]imidazo[l,2-a]pyrazine-8-carboxylate (80 mg, 0.228 mmol) in ‘PrOH (2 mL) and DCM (1 mL) was added ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (174 mg, 0.684 mmol) and DIEA (177 mg, 1.37 mmol). The mixture was stirred at 60 C overnight. Water (5 mL) was added to the mixture and the aqueous layer was extracted with EtOAc (2 X 10 mL). The combined organic layers were washed with water (2 X 10 mL) and brine, dried over anhydrous Na2S04, filtered and concentrated under vacuum. The residue was purified by preparative TLC to afford (R)-methyl 2-(5-(ethoxycarbonyl)-4- (trifluoromethyl)pyrimidin-2-yl)-l-isopropyl-7-(methylsulfonyl)- 1,2,3,4- tetrahydrobenzo[4,5]imidazo[l,2-a]pyrazine-8-carboxylate (75 mg, 57.8% yield) as a yellow solid.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,187035-79-6, its application will become more common.
Reference:
Patent; VITAE PHARMACEUTICALS, INC.; GREGG, Richard, E.; (143 pag.)WO2015/195922; (2015); A1;,
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