Process for the preparation of substituted tetrahydrofolic...

Details Process for the preparation of substituted tetrahydrofolic... Process for the preparation of substituted tetrahydrofolic...

C - Chemistry, Metallurgy

07

D

C07D 475/04 (2006.01)

Patent

CA 2080178

- 1 - "A process for the preparation of substituted tetrahydrofolic derivatives in the6(R,S)(-)] forms and of their active [6(S)(-)]N5 diastereoisomers in form of alkali and earth alkali metal salts." Abstract For the preparation of the [6(R,S)(-)]N5 methyltetrahydrofolic acid and [6(R,S)(-)]N5 formyltetrahydrofolic acids folic acid is hydrogenated with a strong excess of sodium borohydride at temperatures and for times controlled and made different between the admixing steps of the reactants and the true reduction reaction, whereafter the reaction product is treated with formic aldehyde and possibly subjected to a further reduction with NaBH4, if the methyl derivative is desired. By having recourse to the salification with the chloride of an earth alkali metal the therapeutically active 6(S)(-) diastereoisomer is precipitated.

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