Clarithromycin → Clarithromycin formate

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Reaction Steps

Specifically, clarithromycin is dissolved in an organic solvent at a temperature ranging from room temperature to the boiling point of the solvent for a period sufficient to make a solution or suspension. Then, formic acid, neat or dissolved in an organic solvent, is added to the solution or suspension in an amount ranging from 1 to 5 moles based on 1 mole of clarithromycin. The mixture may then be optionally kept at a temperature in the range of room temperature to the boiling point of the solvent for 10 minutes to 1 hour. The resulting mixture is cooled to a temperature in the range of −20° C. to room temperature for a period sufficient to precipitate formate crystals of clarithromycin. Finally, the precipitated crystals are filtered and dried in a conventional manner to give crystalline clarithromycin formate.

Provenance & Evidence