专利号:US-9469614-B2 优先权日:2011-10-27 标 题:Synthesis of triazolopyrimidine compounds 发明人:ZUPANCIC BORUT; MARAS NENAD; STERK DAMJAN 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.
专利号:US-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
专利号:EP-1501848-B1 优先权日:2002-05-08 标 题 :Synthesis of locked nucleic acid derivatives 发明人:SORENSEN MADS DETLEF; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER 权利人:SANTARIS PHARMA AS 摘要:The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as alpha-L-oxy-LNA, amino-LNA, alpha-L-amino-LNA, thio-LNA, alpha-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues. (Formula I)
专利号:US-5350851-A 优先权日:1992-03-16 标题 :Intermediates and a process for synthesis of tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolate and N5-formyl-(6S)-tetrahydrofolate 发明人:BAILEY STEVEN W; AYLING JUNE E 权利人:UNIV SOUTH ALABAMA 摘要:Intermediates and a process for the synthesis of 6-monosubstituted tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolic acid. The intermediates are shown in their two enantiomeric forms as follows: ##STR1## wherein R 1 and R 2 are the same or different and represent hydrogen, methyl, hydroxy, amino, alkyl or dialkylamino, alkoxy, benzyloxy, or benzylthio; R 3 represents an alkene, alkyne, cycloalkyl, benzyl, alkyl (substituted with hydroxy, acetoxy, benzyloxy, alkoxy, alkylthio, amino, carboxy, oxo, or phosphate), a protected aldehyde, or ##STR2## wherein n=1 or 2, R 4 is hydrogen, formyl, methyl, or propargyl, and ZZ represents an amino acid or amino acid polymer.
专利号:US-10131638-B1 优先权日:2018-03-12 标 题:Synthesis of AZO intermediate 发明人:CARUANA PATRICK A; STERN ALFRED G; ZAITA ALEX J; VO THAO 权利人:US NAVY 摘要:A synthesis for an azo intermediate, 5,5′-azobis(4-chloropyrimidine) is disclosed. 5,5′-azobis(4-chloropyrimidine) is a relatively stable azo compound in that decomposition does not occur until about 194° C. 5,5′-azobis(4-chloropyrimidine) is a product of oxidative dimerization of 5-amino-4-pyrimidine, which a water soluble compound. The azo intermediate is formed in an aqueous solution, but the azo intermediate is substantially insoluble in water; and as it forms it separates producing a reaction mixture that is a slurry. The azo intermediate is isolated by filtration. The azo intermediate is marginally soluble in acetone. The yield is at least 18%, and the oxidizing agent (bleach) is inexpensive, reaction conditions do not require extreme heat or cold, which taken together make the azo intermediate suitable for scaling up.
专利号:EP-1105359-B1 优先权日:1998-08-21 标 题:Solid phase synthesis of compounds by carbon-carbon bond forming mitsunobu reactions 发明人:CHATURVEDI SURENDRAKUMAR 权利人:PE CORP NY 摘要:Processes are provided for the Mitsunobu alkylation reaction of carbon-carbon bond formation between a solid support reagent and a reagent in solution. The resulting novel products can be prepared as a combinatorial library by high-throughput, parallel synthesis under robotic automation. Cleaved or support-bound products are useful precursors to biologically active compounds.
[参考文献]: Hongyan Li, Et Al. Regulation Of Photoreceptor Gap Junction Phosphorylation By Adenosine In Zebrafish Retina. Vis Neurosci. 2014 May;31(3):237-43.
合成参考文献
摘要:Granados, A.; Molander, G. A., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 293.