Production of crystalline penem

C - Chemistry – Metallurgy – 07 – D

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C07D 519/00 (2006.01) A61K 31/415 (2006.01)

Patent

CA 2078601

ABSTRACT OF THE DISCLOSURE Disclosed is a method of crystallizing (1R,5S,6S)-2- [(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazolium-6-yl)]thio-6- [(R)-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylate (herein- after simply referred to as L-627), by maintaining an aqueous solution of L-627 at a temperature in the range from the eutectic temperature of the solution to a temperature lower than 0°C. The method provides such advantages that loss of L-627 accompanied by crystallization is reduced, the number of steps in the preparation of vial formulations is small and maintenance of these steps under sterile and dust-free conditions can be per- formed easily, dispensing of the drug can be conducted with quantitative accuracy, and the crystals promptly dissolve in a solvent at the time of use.

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