Synthetic Route of 884495-00-5, 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 884495-00-5 as follows.
Preparation of intermediate (40) All apparatus was flushed with N2 and dried by heating. Reaction under Ar flow.Intermediate (8) (0.00187 mol) was dissolved in degassed TFA (15 ml), then stirred for 4 hours at 85C. The mixture was cooled. The solvent was evaporated in vacuo. The residue was taken up into degassed toluene. The organic layer was separated, washed with a degassed aqueous NaHCO3 solution (2 x 50 ml), dried, filtered and the solvent was evaporated in vacuo to give a yellow foam (*). Under Ar, 4-bromo-5-fiuoro-2- methoxypyridine (1.3 equiv.; 0.50Og) was dissolved in degassed dioxane (10 ml). Cs2CO3 (0.914 g) was added to give suspension (**). A solution of the crude residual oil (*) in degassed dioxane (10 ml) was added to the suspension (**). Then, Pd2(dba)3 (0.029 g) and Xantphos (0.032 g) were added. The resultant brown reaction suspension was stirred overnight at 1000C. The reaction mixture was cooled, and the solvent was evaporated. The residue was dissolved in ethyl acetate, then washed with an aqueous NaHCO3 solution, and once with brine. The organic layer was separated, dried, filtered and the solvent was evaporated. The residue was purified by column chromatography over silica gel. The product fractions were collected and the solvent was evaporated, yielding 0.5113 g of intermediate (40).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,884495-00-5, its application will become more common.
Reference:
Patent; JANSSEN PHARMACEUTICA NV; WO2008/3665; (2008); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem