Preparation process of (6r)-tetrahydro-l-biopterin

Details Preparation process of (6r)-tetrahydro-l-biopterin Preparation process of (6r)-tetrahydro-l-biopterin

C - Chemistry, Metallurgy

07

D

260/242.1

C07D 475/04 (2006.01)

Patent

CA 1262347

ABSTRACT OF THE DISCLOSURE (6R)-Tetrahydro-L-biopterin of the following formula: Image is prepared by catalytically reducing L-erythro- biopterin or an acyl derivative thereof in the presence of an amine, at pH 10 - 13 and with a platinum-base catalyst and when one or more acyl groups still remain, then removing the acyl groups. (6R)-Tetrahydro-L- biopterin is effective for the treatment of certain serious neuroses and malignant hyperphenylalaninemia. The present invention has succeeded in preparing (6R)- tetrahydro-L-biopterin at a high asymmetric ratio R/S and moreover with a high yield. Since the process of this invention makes use of an amine as a base, the process is free from admixture of any inorganic salt and can hence provide high-purity crystals with ease.

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