- Preparation method of sapropterin dihydrochloride
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The invention relates to a preparation method of sapropterin dihydrochloride shown as formula (I) as shown in the specification. The preparation method comprises the steps of taking 5-deoxy arabinoseas a raw material, performing acetylation reaction in the presence of acetic anhydride to form an intermediate DL-1, allowing DL-1 to react with phenylhydrazine under the catalysis of acetic acid to form an intermediate DL-2, allowing DL-2 and pyrimidylamine sulfate to give a ring closing reaction under the catalysis of anhydrous lithium perchlorate to form an intermediate DL-3, directly oxidizingDL-3 through elemental iodine without purification to form an intermediate DL-4, hydrolyzing DL-4 through potassium hydroxide to form L-biopterin (DL-5), and reducing and salifying L-biopterin through a platinum catalyst to form sapropterin dihydrochloride. The preparation method is easy and simple to operate, high in yield, low in energy consumption and suitable for industrial production, the total yield of the preparation method is greater than 70%, and the purity of a final product reaches above 99.5%.
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Paragraph 0025-0026
(2019/06/07)
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- NOVEL PROCESS FOR THE PREPARATION OF SAPROPTERIN DIHYDROCHLORIDE AND ITS KEY INTERMEDIATE, L-BIOPTERIN
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The present invention relates to a novel process for the preparation of Sapropterin dihydrochloride of formula (1) and its key intermediate L-erythro-biopterin of formula (2). The present process is a simple and economically viable process for commercial production of Sapropterin dihydrochloride of formula (1) and its key intermediate L-biopterin of formula (2).
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- COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISEASES
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The invention relates to the compounds of formula I, formula II and formula III or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II or formula III; and methods for treating or preventing metabolic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of phenylketonuria, cardiovascular disease, autism, ADHD, hypertension, endothelial dysfunction and chronic kidney disease.
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- Method for producing L-biopterin
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To provide a method for producing L-biopterin on a large industrial scale by using a reagent which is inexpensive and easy to handle, without requiring a use of any particular equipment or plants.
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Page/Page column 5
(2008/06/13)
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- 169. Pterinechemistry Part 84 A New, Regiospecific Synthesis of L-Biopterin
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Pure L-biopterin was obtained in 42percent yield by the condensation of 5-deoxy-L-arabinose-phenylhydrazone-triacetate with 4-hydroxy-2,5,6-triaminopyrimidine, followed by iodine oxidation of the formed tetrahydropterin derivative to 1',2'-O-diacetyl-L-biopterin.Deacetylation was carried out with NH4OH.
- Schircks, Bernhard,Bieri, Jost H.,Viscontini, Max
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p. 1639 - 1643
(2007/10/02)
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- Pteridines, LXXV. - Synthesis and Properties of Biopterin and Biopterin Analogs
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The synthesis of biopterin (6), its 2-N,N-dimethyl- (8) and 4-thioxo derivative (19) as well as biolumazine (7) is described.The side chain of biopterin can be modified by reaction of α-acetoxy-isobutyryl chloride to yield 6-(L-threo-2-acetoxy-1-chloropropyl)pterin (10), which can be used as a starting material for further derivatisations. 2,1',2'-Triacylbiopterins (14, 16) possess a hydrolytically labile N-acyl group.The newly synthesized compounds were characterized by pK-determinations, UV, and NMR spectra.
- Kappel, Mathias,Mengel, Rolf,Pfleiderer, Wolfgang
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p. 1815 - 1825
(2007/10/02)
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