Electric Literature of 4763-35-3, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.4763-35-3, name is 2-Amino-5-methoxypyrimidin-4(1H)-one, molecular formula is C5H7N3O2, molecular weight is 141.13, as common compound, the synthetic route is as follows.
Step 3. Into a 100 mL round bottom flask equipped with a magnetic stir bar was placed 2-Amino-4-hydroxy-5-methoxy-pyrimidine (500 mg, 3.54 mmol), anhydrous DMF (30 mL), AA-13 (1 .27 g, 5.31 mmol), DBU (2.12 mL, 14.17 mmol), and BOP (1 .96 g, 4.43 mmol). The reaction mixture was allowed to stir at room temperature for 30 minutes then at 50C for 16 hours. The solvent was removed under reduced pressure and the residue was partitioned between brine and ethyl acetate. The organic layers were combined, dried (magnesium sulfate), the solids were removed via filtration, and the solvents of the filtrate were removed under reduced pressure. The crude was purified via reverse phase liquid chromatography (RP Vydac Denali C18 – 10 m, 250 g, 5 cm. Mobile phase 0.25% NH4HCO3 solution in water, methanol), the best fractions were pooled, the solvents were removed under reduced pressure to afford 89.
The chemical industry reduces the impact on the environment during synthesis 4763-35-3, I believe this compound will play a more active role in future production and life.
Reference:
Patent; JANSSEN R&D IRELAND; MC GOWAN, David; RABOISSON, Pierre Jean-Marie Bernard; EMBRECHTS, Werner; JONCKERS, Tim, Hugo, Maria; LAST, Stefaan, Julien; PIETERS, Serge, Maria, Aloysius; VLACH, Jaromir; WO2012/136834; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia