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1301214-63-0

5-(1H-IMidazol-1-yl)picolinic acid synthesis

3synthesis methods
2-Pyridinecarbonitrile, 5-(1H-imidazol-1-yl)-

1301214-64-1
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5-(1H-IMidazol-1-yl)picolinic acid

1301214-63-0
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Yield:1301214-63-0 84%

Reaction Conditions:

Stage #1: 5-(1H-imidazol-1-yl)picolinonitrilewith hydrogenchloride;water for 2 h;Reflux;
Stage #2: with pyridine in water;

Steps:

6 5-(1H-imidazol-1-yl)picolinic acid

5-(1H-imidazol-1-yl)picolinonitrile (136 mg, 0.80 mmol) was heated to reflux in 6N aqueous hydrochloric acid (10 mL) for 2 hours. The reaction mixture was evaporated and the residue was azeotroped with three portions of toluene to give a residue which was purified on an ion exchange column (AG-50 Biorad) eluting with a 0-10% pyridine in water gradient to give the title compound as a white solid (128 mg, 84%). 1H NMR (400 MHz, DMSO-d6) δ ppm 9.10 (s, 1H), 8.50 (s, 1H), 8.26-8.33 (m, 1H), 8.13-8.20 (m, 1H), 7.96 (s, 1H), 7.16 (s, 1H).

References:

US2011/111046,2011,A1 Location in patent:Page/Page column 14