Method of production of d,l-5-methyltetrahydrofolic acid and its alkali and alkali salts

摘要

Process for the preparation of d,l-5-methyltetrahydrofolic acid and its salts of the formula 1 in which X is hydrogen, an alkali metal or the equivalent of an alkaline earth metal, by reduction of folic acid with NaBH4 and methylation of the tetrahydrofolic acid obtained with aqueous solutions of formaldehyde and sodium borohydride in an inert gas atmosphere. The process is simple and can be carried out without separation of intermediates while carrying out the process steps successively in the same reaction vessel. The final products are obtained in a yield of more than 80%, relative to folic acid employed, in a purity of more than 99%. The compounds of the formula I obtained are non-toxic, stable at physiological pH and suitable for the preparation of liquid or solid pharmaceutical compositions for any type of application in human therapy. Such compositions exhibit haematopoietic action, hepatoprotective and antineoplastic action. IMAGE