专利号:US-6639059-B1 优先权日:1999-03-24 标 题 :Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.
专利号:US-9334273-B1 优先权日:2014-03-05 标题:Efficient and stereoselective synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) 发明人:CHU DAVID C K; SINGH UMA S 权利人:UNIV GEORGIA 摘要:The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) from a readily available starting material (Vince lactam) in fourteen steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, D -2′-fluoro-6′-methylene cyclopentanol by diazotization, elimination, stereoselective epoxidation, fluorination and oxidative reduction of the Vince lactam in twelve steps is also provided.
专利号:EP-0948511-B1 优先权日:1996-12-24 标 题:Chemical synthesis of nucleosides analogs and their incorporation into polynucleotides 发明人:KARPEISKY ALEXANDER; BEIGELMAN LEONID; MATULIC-ADAMIC JASENKA 权利人:SIRNA THERAPEUTICS INC 摘要:Novel nucleosides, process for chemical synthesis of nucleosides and incorporation of the nucleosides into polynucleotides are disclosed. Also described are polynucleotides, such as antisense, TFO and nucleic acid catalysts with one or more modifications, such as 2'-O-amino, L-nucleotides and the others.
专利号:US-5324831-A 优先权日:1988-04-06 标题:Phosphoramidite reagent for chemical synthesis of modified DNA 发明人:MARQUEZ VICTOR E; GODDARD AMANDA J 权利人:US HEALTH 摘要:5,6-dihydro-5-azacytidine phosphoramidite is useful in the synthesis of oligonucleotides and DNA containing dihydro-5-aza- and 5-azacytosine bases. The modified oligonucleotides which contain 5-azacytosine residues at specific sites can be used to determine the mechanism of selective gene activation and the relationship existing between the presence of the triazine base and inhibition of DNA methylation.
专利号:US-6972330-B2 优先权日:1996-02-13 标题:Chemical synthesis of methoxy nucleosides 发明人:BEIGELMAN LEONID; HAEBERLI PETER; KARPEISKY ALEXANDER; SWEEDLER DAVID 权利人:SIRNA THERAPEUTICS INC 摘要:Process for chemical synthesis of methoxy nucleosides.
专利号:US-7342003-B2 优先权日:2001-10-25 标 题 :Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs 发明人:MOORMAN ALLAN R; SCANNELL MICHAEL; BALASUBRAMANIAN THIAGARAJAN; OUTCALT RUSSELL; LEUNG EDWARD 权利人:KING PHARMACEUTICALS RES & DEV 摘要:Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.
参考标题:Synthesis Of Phosphatidyl-β-Glucosyl Glycerol Containing A Dioleoyl Diglyceride Moiety 作者:C.A.A. Van Boeckel,G.M. Visser,J.H. Van Boom |发布日期:1985.1 摘要:In A Two Step Procedure, To Afford Compound ; (C) A 2,4-Dichlorophenyl Protected Phosphatidic Acid Derivative . Compound Could Be Selectively Coupled To The Primary Hydroxyl Function Of To Afford The Fully Protected Glycophospholipid . Finally, Removal Of The 2,4-Dichlorophenyl And Tips Protecting Groups From Was Performed With Syn-4-Nitrobenzaldoximate And Fluoride Ions, Respectively, To Afford Glycophospholipid
合成参考文献
摘要:Yoshimatsu, M., Science of Synthesis Knowledge Updates, (2016) 2, 394.