Process for the preparation of optically pure...

C - Chemistry – Metallurgy – 12 – P

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C12P 7/40 (2006.01) C07D 475/04 (2006.01) C12N 9/00 (2006.01) C12P 7/62 (2006.01) C12P 17/18 (2006.01) C12P 41/00 (2006.01)

Patent

CA 2031784

A process for the preparation of optically pure diastereoisomers of tetrahydrofolate compounds is described, comprising the conversion, for example, of only the 5,6S,7,8-tetrahydrofolic acid component of a racemic mixture of 5,6,7,8-tetrahydrofolic acid to 10-formyl-5,6S,7,8-tetrahydrofolic acid in the presence of a formyl tetrahydrofolate synthetase, followed by cyclizing, hydrolyzing and derivatizing. The process is also useful to make a desired substantially pure (6R or 6S) enantiomer of a derivative or (radiolabeled) tetrahydrafolic acid or a salt or ester thereof.

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