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914637-28-8

2-(1H-IMIDAZOL-1-YL)ISONICOTINIC ACI synthesis

1synthesis methods
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Yield:914637-28-8 98%

Reaction Conditions:

with copper(l) iodide;caesium carbonate in dimethyl sulfoxide at 125; for 18 h;

Steps:

52a Example 52a: 2-(1H-imidazol-1-yl)isonicotinic acid

To a solution of 2-bromoisonicotinic acid (1.87 g, 9.26 mmol), 1H-imidazole (573mg, 8.42 mmol) and Cs2C03 (6.03 g, 18.5 mmol) in DMSO (18.6 mL), was added Cui (176mg, 0.926 mmol). The mixture was heated to 125°C, stirred for 18 hours, cooled to room10 temperature, filtered and purified by preparative HPLC (1 0-90% acetonitrile in water) to givethe title compound as a light pink solid (1. 72 g, 98% ). MS 190 (MH+).

References:

WO2014/25706,2014,A1 Location in patent:Page/Page column 103