Introduction of a new synthetic route about 2-Amino-8-bromo[1,2,4]triazolo[1,5-a]pyridine

According to the analysis of related databases, 1124382-72-4, the application of this compound in the production field has become more and more popular.

Electric Literature of 1124382-72-4, Adding some certain compound to certain chemical reactions, such as: 1124382-72-4, name is 2-Amino-8-bromo[1,2,4]triazolo[1,5-a]pyridine,molecular formula is C6H5BrN4, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 1124382-72-4.

Intermediate 49 (16 g, 55.92 mmol) and water (75 mL) were added to a sol. of intermediate 51 (7.94 g, 37.28 mmol) in DME (200 mL). Then, Pd(PPh3)4 (4.31 g, 3.73 mmol) was added and the r.m. was stirred at 150 C for 10 min. under microwave irradiation. The mixture was filtered through diatomaceous earth and concentrated in vacuo. The crude product was purified by flash column chromatography (silica; eluent: DCM/(7 N NH3 in MeOH) from 100/0 to 97/3). The product fractions were collected and the solvent evaporated in vacuo to yield 7 g of a first fraction of intermediate 52. The impure fractions were also collected, evaporated in vacuo and the crude product was purified by RP preparative HPLC [RP Vydac Denali CI 8 (10 mm, 250 g, 5 cm); mobile phase: 0.25% NH4HC03 sol. in water/CH3CN]. The product fractions were collected and the solvent evaporated in vacuo. The crude product was further purified by RP preparative SFC [Diol; mobile phase: C02, MeOH (with 0.2% isopropylamine)]. The product fractions were collected and the solvent evaporated in vacuo to yield 4 g of a second fraction of intermediate 52. Yield: 11 g of intermediate 52 (quantitative yield).

According to the analysis of related databases, 1124382-72-4, the application of this compound in the production field has become more and more popular.

Reference:
Patent; JANSSEN PHARMACEUTICALS, INC.; MINNE, Garrett, Berlond; BISCHOFF, Francois Paul; GIJSEN, Henricus, Jacobus, Maria; VELTER, Adriana, Ingrid; PIETERS, Serge, Maria, Aloysius; BERTHELOT, Didier, Jean-Claude; WO2013/10904; (2013); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem