Method for making pure stereoisomers of tetrahydrofolic acid...

C - Chemistry – Metallurgy – 07 – D

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C07D 475/04 (2006.01) C07D 239/00 (2006.01) C07D 241/00 (2006.01)

Patent

CA 2378869

A process for preparing and concentrating (6S,.alpha.S) or (6S,.alpha.R) tetrahydrofolic acid ester salts and (6S,.alpha.S) or (6S,.alpha.R) tetrahydrofolic acid, characterised by preparing or dissolving equimolar or concentrated mixtures of diastereomers of addition salts of tetrahydrofolic acid esters with aromatic sulphonic acids in organic solvents, followed by crystallising them at least once, and then if applicable hydrolysing the crystallisate to produce (6S,.alpha.S) or (6S,.alpha.R) tetrahydrofolic acid, crystallising the latter as a free acid or isolating it in the form of a salt.

L'invention concerne un procédé de fabrication et d'enrichissement de sels d'esters d'acide (6S, alpha S)- ou (6S, alpha R)-tetrahydrofolique et d'acide (6S, alpha S)- ou (6S, alpha R)-tetrahydrofolique, caractérisé par le fait qu'on produise ou dissolve des mélanges équimolaires ou enrichis de diastéréomères de sels addition d'esters d'acide tetrahydrofolique avec des acides sulfoniques aromatiques dans des solvants organiques, qu'on les cristallise ensuite au moins une fois, que le produit de la cristallisation soit hydrolisé en acide (6S, alpha S)- ou (6S, alpha R)-tetrahydrofolique le cas échéant, qu'on cristallise ce dernier en tant que qu'acide libre ou qu'on l'isole sous forme d'un sel.

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