- METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE
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Disclosed is a method for synthesizing sapropterin dihydrochloride. The present invention reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
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- METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE
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Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
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Paragraph 0058; 0059
(2015/05/05)
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- METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE
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Disclosed is a method for synthesizing sapropterin dihydrochloride. The present invention reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
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Paragraph 0025
(2015/03/03)
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- METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE
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Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
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Paragraph 0053
(2015/04/22)
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- Synthesis of (-)-Biopterin Using (S)-Ethyl Lactate as a Starting Material
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(-)-Biopterin was synthesized from (1S,2S)-1-(1,3-dithian-2-yl)propane-1,2-diol 5 (=C), which was derived from commercially available (S)-ethyl lactate.Diol 5 (=C) was converted to 15 through a six-step sequence.Ketone 15 was submitted to condensation with 3,5,6-triaminopyrimidinol (TAP, 2), and followed by oxidation to afford isopropylidenebiopterin (16).Finally, 16 was deprotected to give (-)-biopterin (1).
- Kikuchi, Haruhiko,Mori, Kenji
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p. 2095 - 2100
(2007/10/02)
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- ENZYMATIC ENANTIOSELECTIVE HYDROLYSIS OF 2,2-DIMETHYL-1,3-DIOXOLANE-4-CARBOXYLIC ESTERS
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2,2-dimethyl-1,3-dioxolane-4-carboxylic acid derived chiral building blocks were prepared from substituted α,β-unsaturated acids with high enantiomeric purities by enzymatic hydrolysis of their n.butyl esters.
- Pottie, M.,Eycken, J. Van der,Vandewalle, M.,Dewanckele, J. M.,Roeper, H.
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p. 5319 - 5322
(2007/10/02)
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- Substituted 5-(D,L-erythro-1',2'-Dihydroxypropyl)pyrazines. Potential Precursors for the Synthesis of Biopterin Derivatives
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A convenient synthesis of substituted 5-(D,L-erythro-1',2'-dihydroxypropyl)pyrazines from crotonic acid 4 is described.The anomalous behavior during decarboxylation of functionalized 2-oximino-3-oxoesters 8a,b is noted.The structures of prepared compounds
- Pastor, Stephen D.,Nelson, Aaron L.
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p. 657 - 660
(2007/10/02)
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