Synthetic Progress on Sapropterin Hydrochloride and Its Raw Material Biopterin
Phenylketonuria is a rare autosomal recessive disease caused by phenylalanine metabolism disorders.In most cases,phenylketonuria results from a lack of phenylalanine hydroxylase due to mutations in the phenylalanine hydroxylase gene.Sapropterin hydrochloride was approved by the US FDA in December 2007 and is the only drug used in the treatment of phenylketonuria responsive to tetrahydrobiopterin.However,the synthesis of Sapropterin hydrochloride is hard due to its complex molecular structure,difficulty in the chirality control.Herein,the synthesis of Sapropterin hydrochloride and its key raw material biopterin were reviewed.
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