Process for the preparation of alkaline earth metal salts of (6R)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid
AssigneeSapec S.A. fine chemicals
InventorsAttilio Melera, Fabrizio Marazza
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Abstract
A process for the preparation of alkaline earth metal salts of (6R)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid. An alkaline earth metal salt, either in the form of a solid, or in the form of an aqueous solution, is added, preferably under an inert gas atmosphere, to an ammonium salt or alkali metal salt of (6RS)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid dissolved in water or an aqueous buffer solution. II is added an alkaline earth metal salt either in the form of a solid or in the form of an aqueous solution. The obtained mixture is allowed to crystallize, and the obtained solid is separated. The product is known to be cytostatic.
Claims10
A process for preparing an alkaline earth metal salt of (6R)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid of the following formula (I):
- ##STR3## wherein Y is Ca.sup.2+ or Mg.sup.2+, said process comprising:
- (i) under an inert atmosphere and temperature conditions of about 20.degree. C. to about 60.degree. C., adding a calcium or magnesium halide or acetate, either in the form of an aqueous solution or a solid, to an ammonium salt of, or alkali metal salt of, (6RS)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid dissolved in water or in an aqueous buffer solution, said salt of (6RS)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid having the following formula (II):
- ##STR4## wherein X is an alkali metal cation or NH.sub.4.sup.+ ;
- (ii) under temperature conditions of about 20.degree. C. to about 40.degree. C., allowing the mixture obtained from step (i) to crystallize;
- and
- (iii) separating a solid obtained from step (ii), said solid characterized by formula (I).
Dependencies are inferred from the claim text.