专利号:US-8912319-B2 优先权日:2010-07-15 标 题 :Synthesis of 2′-deoxy-2′-[18F]fluoro-5-methyl-1-B-D-arabinofuranosyluracil (18F-FMAU) 发明人:LI ZIBO; CAI HANCHENG; CONTI PETER S 权利人:LI ZIBO; CAI HANCHENG; CONTI PETER S; UNIV SOUTHERN CALIFORNIA 摘要:The present invention relates to methods of synthesizing 18 F-FMAU. In particular, 18 F-FMAU is synthesized using one-pot reaction conditions in the presence of Friedel-Crafts catalysts. The one-pot reaction conditions are incorporated into a fully automated cGMP-compliant radiosynthesis module, which results in a reduction in synthesis time and simplifies reaction conditions. The one-pot reaction conditions are also suitable for the production of 5-substituted thymidine or cytidine analogs. The products from the one-pot reaction (e.g. the labeled thymidine or cytidine analogs) can be used as probes for imaging tumor proliferative activity. More specifically, these [ 18 F]-labeled thymidine or cytidine analogs can be used as a PET tracer for certain medical conditions, including, but not limited to, cancer disease, autoimmunity inflammation, and bone marrow transplant.
专利号:US-4914233-A 优先权日:1988-03-01 标题:Synthesis of beta-thymidine 发明人:FRESKOS JOHN N; SENARATNE K PUSHPANANDA A 权利人:ETHYL CORP 摘要:A process is provided in which a mixture of alpha- and beta-anomers is converted selectively to the desired beta-thymidine. The process involves the following steps: (a) converting a mixture of alpha- and beta-anomers of tetra-O-acylribofuranose to tri-O-acyl-β-ribothymidine; (b) converting tri-O-acyl-β-ribothymidine to β-ribothymidine; (c) converting β-ribothymidine to 2,2'-anhydro-β-thymidine; (d) converting 2,2'-anhydro-β-thymidine to 2'-halo-2'-deoxy-5-methyluridine; and (e) converting 2'-halo-2'-deoxy-5-methyluridine to beta-thymidine. The mixture of alpha- and beta-anomers of tetra-O-acylribofuranose may be produced by any suitable procedure such as by converting lower alkyl ribofuranoside to the tetra-O-acylribofuranose mixture. The lower alkyl ribofuranosides may in turn be produced by various methods. However, a desirable way of effecting this conversion involves use of D-ribose as the starting material which is converted to the lower alkyl ribofuranoside.
专利号:US-2023416293-A1 优先权日:2020-11-23 标 题:Synthesis of [18f]-labeled thymidine analogues 发明人:CHEN KAI; CONTI PETER S 权利人:UNIV SOUTHERN CALIFORNIA 摘要:Thymidine analogues, 5-substituted 2′-deoxy-2′-[18F]fluoro-arabinofuranosyluracil derivatives, are promising positron emission tomography (PET) tracers being evaluated for noninvasively imaging cancer cell proliferation and/or reporter gene expression. We report the radiosynthesis of 2′-deoxy-2′-[18F]fluoro-5-methyl-1-β-d-arabinofuranosyluracil ([18F]FMAU) and other 2′-deoxy-2′-[18F]fluoro-5-substituted-1-β-d-arabinofuranosyluracil analogues using 1,4-dioxane to replace the currently used 1,2-dichloroethane. Compared to 1,2-dichloroethane, 1,4-dioxane is analyzed as a better solvent in terms of radiosynthetic yield and toxicity concern. The use of a less toxic solvent allows for the translation of the improved approach to clinical production. The new radiolabeling method can be applied to an extensive range of uses for 18F-labeling of other nucleoside analogues.
专利号:US-4987224-A 优先权日:1988-08-02 标 题 :Method of preparation of 2',3'-dideoxynucleosides 发明人:CHU CHUNG K 权利人:UNIV GEORGIA RES FOUND 摘要:A general method of synthesis of 2',3'-dideoxynucleosides which is efficient, inexpensive and based on a readily available starting material, D-mannitol.
专利号:SU-1643553-A1 优先权日:1989-05-23 标题:1, 5-di-o-benzoyl-3-fluoro-2, 3-dideoxy-d- ribofuranose as semiproduct in stereospecific synthesis of 3- fluoro-2, 3- dideoxytimidine
专利号:US-2012053337-A1 优先权日:2010-07-15 标 题 :SYNTHESIS OF 2'-Deoxy-2'-[18F]FLUORO-5-METHYL-1-B-D-ARABINOFURANOSYLURACIL (18F-FMAU)
参考标题:Synthetic Approaches To Novel Cis And Trans Dideoxynucleosides Of The Apiose Family 作者:Todd B. Sells,Vasu Nair |发布日期:1994.4 摘要:Stereoselective Synthesis Of The Complete Family Of Optically Active Dideoxygenated Nucleosides Of The Apiose Family Have Been Developed. The Chiral Aldodiol System 7, A Key Intermediate In This Synthesis, Was Prepared From The Prochiral Molecule 6, Through The Action Of The Lipase From Candida Cylindracia. Approaches To Novel Enantiomeric And Diastereoisomeric Dideoxynucleosides Containing The Te
合成参考文献
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