Preparation method of L-erythro biopterin

A technology of biopterin and erythrotype, which is applied in the field of preparation of L-erythrotype biopterin, can solve the problems of strong odor and long reaction cycle, and achieve the effect of short cycle, easy operation and mild reaction conditions
CN101792445BInactive Publication Date: 2012-05-30BEIJING INSTITUTE OF TECHNOLOGYGY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
BEIJING INSTITUTE OF TECHNOLOGYGY
Publication Date
2012-05-30
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a preparation method of L-erythro biopterin used as a preparation intermediate body of a clinically used medicament (R)-2-amido-6-[(1R, 2S)-1,2-dihydroxy propyl]-5,6,7,8-tetrahydro-4(3H)-pteridine ketone hydrochloride for treating atypical hyperphenylalaninemia, which belongs to the technical field of medicinal chemistry. The preparation method sequentially comprises the steps of: reacting L-(+)-arabinose 1 with alkyl hydrosulfide by acetalization; adding sulfonyl chloride for generating a sulfonation reaction; reducing and removing sulfonyl ester; removing reduced sulfur aldehyde protective groups; reacting with hydrazine for obtaining a hydrazine compound; reacting with estolide or the sulfonyl chloride; reacting with 2,4,5-3-amino-pyrimidine ketone; adding an oxidant; and removing acyl for obtaining the L-erythro biopterin. The invention ensures deodorizing equipment is not installed on a reaction system by utilizing Odourless mercaptan, thereby saving costand optimizing a working environment; and the invention has mild reaction condition of each step, short period and easy operation.
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Description

technical field

[0001] The invention relates to a preparation method of L-erythrobiopterin, which is used as a clinically used therapeutic drug for atypical hyperphenylalaninemia (R)-2-amino-6-[(1R,2S)-1,2 -dihydroxypropyl]-5,6,7,8-tetrahydro-4(3H)-pteridone hydrochloride (common name: Sapropterin hydrochloride (Sapropterin hydrochloride)) preparation intermediate L-erythro The invention discloses a method for preparing type biopterin, which belongs to the technical field of medicinal chemistry. Background technique

[0002]

[0003] Chemical formula I represents that L-erythro-biopterin is a kind of pteridines widely existing in nature.

[0004]

[0005] Chemical formula II represents (R)-2-amino-6-[(1R, 2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydro-4(3H)-pteridone ( BH4) is an essential coenzyme in hydroxylation reaction and oxygenase in organisms, and is the most important coenzyme of nitric oxide synthase (NOS); sapropterate hydrochloride is a drug approved by many...

Claims

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