C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 477/20 (2006.01) A61K 31/407 (2006.01) A61P 31/04 (2006.01)
Patent
CA 2457642
A process for preparing a crystalline, carbapenem monosodium salt of formula IIa, characterized by the steps a) adding about 10 to 30 % of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than -5 ~C, c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between -5 and -25 ~C.
L'invention concerne un procédé de préparation d'un sel monosodique, cristallin, de carbapénème de formule IIa, consistant a) à ajouter environ 10 à 30 % d'un solvant organique à une solution aqueuse du carbapénème, b) à refroidir la solution résultante à une température inférieure à -5 ·C, c) à ajuster le pH à l'aide d'une solution contenant un acide dans un solvant organique afin de donner le pH correct pour la cristallisation, et d) à faire cristalliser le composé par addition de méthanol et d'un alcool en C¿2-5? entre -5 et -25 ·C.
Brands Karel M. J.
Crocker Louis S.
Cvetovich Raymond
Fisher Elizabeth S.
Jobson Ronald
Merck & Co. Inc.
Merck Sharp & Dohme Corp.
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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