Crystalline solid form of...

C - Chemistry – Metallurgy – 07 – C

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C07C 257/14 (2006.01) A61K 31/155 (2006.01) A61P 29/00 (2006.01)

Patent

CA 2494583

(2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid is crystallized as an anhydrous, stoichiometric 1.5 HCl salt and a scaleable crystallization method is disclosed. The salt form was characterized and the absolute configuration of the chiral center was confirmed as "S". (2S,5Z)-2- amino-7-(ethanimidoylamino)-2-methylhept-5~enoic acid was high melting and appears acceptably non-hygroscopic for use in a pharmaceutical composition.

L'invention porte sur l'acide (2S,5Z)-2-amino-7-(éthanimidoylamino)-2-méthylhept-5-énoïque cristallisé en tant que sel anhydride d'HCl à stoechiométrie de 1,5 et sur un procédé extensible de cristallisation. On a caractérisé la forme du sel et confirmé la configuration absolue du centre chiral qui est en "S". L'acide (2S,5Z)-2-amino-7-(éthanimidoylamino)-2-méthylhept-5-énoïque présente un point de fusion élevé et une non hygroscopicité acceptable pour pouvoir l'utiliser dans une préparation pharmaceutique.

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