4-(2-bromoanilino)pyridine synthesis

Yield:86775-99-7 99%

Reaction Conditions:

with 1,1'-bis-(diphenylphosphino)ferrocene;tris-(dibenzylideneacetone)dipalladium⁽⁰⁾;sodium t-butanolate in toluene at 120; for 18 h;Sealed tube;

Steps:

1.2.i (i) Synthesis of 4-(2'-Bromoanilino)pyridine

To a sealed tube equipped with a magnetic stir bar was added 4-aminopyridine (944 mg, 10.0 mmol), t-BuONa (1.14 g, 11.9 mmol), tris (dibenzylideneacetone) -dipalladium (137 mg, 0.150 mmol),And 1,10-bis (diphenylphosphino) ferrocene (200 mg, 0.361 mmol).The resulting mixture was stirred at 120 for 18 hours.The reaction mixture was cooled to ambient temperature.The mixture was filtered through a pad of celite and washed with CH2Cl2.The filtrate was concentrated in vacuo and 4- (2'-Bromoanilino) pyridine was synthesized (2.48 g, 99% yield) by column chromatography (3% MeOH in CH2Cl2 followed by 10% MeOH in CH2Cl2).

References:

KR2019/22316,2019,A Location in patent:Paragraph 0346; 0347; 0361-0364