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ChemicalBook CAS DataBase List Metronidazole
443-48-1

Metronidazole synthesis

8synthesis methods
Metronidazole, 2-methyl-5-nitroimidazol-1-ethanol (37.2.10), is made by nitrating 2-methylimidazole to make 2-methyl-5-nitroimidazole (37.2.9), which is then reacted with 2-chloroethanol or ethylenoxide, which is easily transformed to the desired metronidazole.

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Yield:443-48-1 88%

Reaction Conditions:

with formic acid;sulfuric acid at 80; for 12 h;Temperature;

Steps:

3.1

(1) with a thermometer,Stirrer and airway in the reaction vessel were added formic acid 100mg,Concentrated sulfuric acid 20mg,Prepared into mixed acid solution,To the mixed acid solution was added 2-methyl-5-nitroimidazole (25 mg)Another take a couple of reaction bottles,Add 5 ml of ethylene oxide,Unicom reaction system, the reaction vessel slowly into the ethylene oxide,After reaction at 80 ° C for 12 h,Add the appropriate amount of 1M sodium hydroxide solution to the reaction solution to adjust the pH to 8,Add 5ml ethyl acetate solvent extraction three times, combined withThe phases were dried over anhydrous sodium sulfate and filtered,The filtrate was evaporated under reduced pressure to give metronidazole 29.5 mg in a yield of 88%.

References:

CN106674123,2017,A Location in patent:Paragraph 0044; 0045

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