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2-(pyridin-3-yl)pyridin-3-amine synthesis

5synthesis methods
-

Yield: 44%

Reaction Conditions:

with tetrakis(triphenylphosphine) palladium(0);potassium carbonate in 1,4-dioxane;water at 120; for 8 h;Inert atmosphere;

Steps:

26.1 1,Synthesis of intermediate 2-(2-methoxyphenyl)pyridine-3-amino(Step a):
General procedure: Weigh out 2-bromo-3-aminopyridine (1,500mg)With 2-methoxyphenylboronic acid (483mg, 1.1eq)Dissolved in toluene/water mixed solvent (2/1, v/v),Add potassium carbonate (1.6g, 4eq)And Pd(PPh3)4 (167mg, 0.05eq)As a catalyst,The reaction flask is at 80°C under nitrogen atmosphere,The reaction was terminated after stirring for 8 hours.The solvent was distilled off under reduced pressure and extracted with ethyl acetate/water for 3 times. The ethyl acetate layer was taken out, spin-dried, and purified by silica gel column chromatography to obtain the intermediate 2-(2-methoxyphenyl)pyridine-3- Amino (310mg, yield 60%).

References:

Zhejiang University;Pan Yuanjiang;Zhu Heping;Jin Hongchuan;Ying Shilong;Liang Xiao CN111320575, 2020, A Location in patent:Paragraph 0036; 0037; 0130; 0131