Preparation process of (6R)-tetrahydro-l-biopterin.

摘要

@ (6R)-Tetrahydro-L-biopterin of the following formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="24" wi="60" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>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 hyperphenylalaniemia. 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.