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1H-BenziMidazole-5-carboxylic acid, 2-aMino-1-Methyl-, Methyl ester synthesis

3synthesis methods
-

Yield:1258070-65-3 96%

Reaction Conditions:

in tetrahydrofuran;water at 20 - 50; for 4 h;

Steps:

4.A.II; 4.A.III

(II) A solution of the product just obtained in stage (II) (4.4 mmol) in water (10 ml) was added cyanogen bromide (5.28 mmol) in THF (4 ml) and water (30 ml) at room temperature and the reaction mixture was stirred at 50 0C for 4 h. The reaction mixture was diluted with ethyl acetate and the organic phase was washed with water and sat. NaCI solution, dried over Na2SO4 and concentrated. The crude product was recrystallized from methanol / diethyl ether. Yield: 96 %

References:

WO2010/142402,2010,A1 Location in patent:Page/Page column 112