New downstream synthetic route of 884495-00-5

With the rapid development of chemical substances, we look forward to future research findings about 884495-00-5.

The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 884495-00-5, name is 4-Bromo-5-fluoro-2-methoxypyridine. This compound has unique chemical properties. The synthetic route is as follows. name: 4-Bromo-5-fluoro-2-methoxypyridine

Example A.18 Preparation of [0214] [0215] 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 85 C. 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 (2×50 ml), dried, filtered and the solvent was evaporated in vacuo to give a yellow foam (*). Under Ar, 4-bromo-5-fluoro-2-methoxypyridine (1.3 equiv.; 0.500 g) 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 100 C. 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).

With the rapid development of chemical substances, we look forward to future research findings about 884495-00-5.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; Gijsen, Henricus Jacobus Maria; De Cleyn, Michel Anna Jozef; Surkyn, Michel; Verbist, Bie Maria Pieter; US2013/324529; (2013); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem