专利号:EP-1108724-B1 优先权日:1996-01-16 标题 :Synthesis of methoxy nucleosides and enzymatic nucleic acid molecules 发明人:WINCOTT FRANCINE; BEIGELMANN LEONID; MATULIC-ADAMIC JASENKA; USMAN NASSIM; HAEBERLI PETER; KARPEISKY ALEXANDER; SWEEDLER DAVID; JARVIS THALE; DIRENZO ANTHONY 权利人:SIRNA THERAPEUTICS INC 摘要:This invention relates to chemical synthesis of 2'-O-methyl, 3'-O-methyl and 5'-O-methyl nucleosides, incorporation of novel chemical modifications in enzymatic nucleic acid molecules and improved methods for the synthesis of enzymatic nucleic acid molecules.
专利号:EP-1992632-A1 优先权日:2007-05-12 标题 :Method for the synthesis of cyclouridine 发明人:MOCIARDINI SIMONE; COLOMBO PAOLO 权利人:EXPLORA LAB SA 摘要:Method for the synthesis of possibly substituted cyclic derivatives of uridine, of formula (II)n nwherein R is chosen in the group that comprises: hydrogen, halogen and C 1-4 alkyl, the method comprising the step of reacting a possibly substituted uridine of formula (III)n nwherein R has the same meanings as in formula (II), and glycerol carbonate in the presence of an alkaline carbonate at a temperature of 70°C-130°C.
专利号:US-9751909-B2 优先权日:2011-09-07 标 题 :Synthesis and uses of nucleic acid compounds with conformationally restricted monomers 发明人:MATRAY TRACY J; MACIAGIEWICZ IWONA M; HOUSTON JR MICHAEL E 权利人:MATRAY TRACY J; MACIAGIEWICZ IWONA M; HOUSTON JR MICHAEL E; MARINA BIOTECH INC 摘要:Processes for synthesis of conformationally restricted nucleomonomers (CRN) by ozonolysis or oxidation of a 2′-vinyl substituted nucleoside precursor with protected 3′-hydroxyl, 4′-hydroxymethyl and 5′-hydroxyl positions. The CRN nucleomonomers can be used to prepare nucleic acid compounds. CRN nucleomonomers for nucleic acid compounds can be prepared in high yields and in multi-gram scale. The nucleic acid compounds can be of various regulatory classes such as antisense RNA for therapeutic modalities useful for treating or preventing diseases or disorders by up- or down-regulating the expression of genes and other nucleic acid based regulatory systems in a cell.
专利号:US-8691789-B2 优先权日:2012-08-30 标 题 :Probe of iodine-123 marker thymidine (FLT)analogue [123I]-IaraU 发明人:CHEN JENN-TZONG; HUANG HO-LIEN; CHEN JIA-RONG; YU CHUNG-SHAN; SU WEN-CHIN; YANG CHING-SHIUANN; LIN WUU-JYH 权利人:ATOMIC ENERGY COUNCIL; INST NUCLEAR ENERGY RES ATOMIC ENERGY COUNCIL 摘要:A tumor radiation probe of iodine-123 marker thymidine (FLT) analogue [ 123 I]-IaraU is disclosed. Commercial available uridine is used as the raw material for the synthesis of the precursor. A radioactive iodine-123 is marked on an alkaline group of uridine to obtain [ 123 I]-IaraU, which is distinguishable from [ 18 F]-FLT marking 18 F on a glycosyl group to obtain a novel tumor radiation probe. The marking procedures include mixing the marker precursor with Na [ 123 I] solution, acetic acid and hydrogen peroxide solution, and the solution of chloroform and sodium hydroxide. The sonication time increases from 1 minute to 10 minutes, so that [ 123 I]-IaraU has radiologically chemical purity of higher than 98% and radiological specific activity of not less than 0.196 GBq/umole, and the yield can increase from 8% to 40%. Its radioactive specific activity, yield and purity reach to the degree for the use in biological experiments, while reducing production cost.
专利号:US-3856777-A 优先权日:1971-12-14 标题:Method of producing pyrimidine nucleoside derivatives 发明人:ISHIDO Y; YOSHINO T; YAMASAKI A; OKUTSU M; KOMURA H; SUZUKI K 权利人:AJINOMOTO KK 摘要:Uridine, cytidine, and derivatives thereof arrived at by substitution in positions 4, 5 and 5'' are converted to the corresponding 2,2''-anhydro compounds by reaction with cyclic lower alkylene and alkenylene esters of carbonic acid. The anhydro compounds are hydrolyzed to arabinofuranosylpyrimidine derivatives in a basically known manner. The latter as well as the anhydro compounds are known physiologically active agents and/or intermediates in the synthesis of such agents.
专利号:US-8394934-B2 优先权日:2008-03-21 标 题:Method and process for synthesis of 2',3'-didehydro-2',3'-dideoxynucleosides 发明人:HUANG ZHEN; SHENG JIA 权利人:HUANG ZHEN; SHENG JIA 摘要:A method is disclosed for synthesizing 2′,3′-didehydro-2′,3′-dideoxynucleosides (d4Ns) from a nucleophile-mediated elimination, such as a telluride-mediated elimination reaction. After substitution of 2,2′-anhydronucleosides with a nucleophile, such as a telluride monoanion, a telluride intermediate is formed, and its elimination leads to formation of the olefin products (d4Ns). This disclosure describes this telluride-assisted (or nucleophile-assisted) reaction and how to facilitate the substitution and elimination in order to form d4Ns.
参考文献:10.1021/ol049366x 摘要:Dai Q, Piccirilli JA. Efficient synthesis of 2',3'-dideoxy-2'-amino-3'-thiouridine. Org Lett. 2004 Jun 24;6(13):2169–72. doi: 10.1021/ol049366x. 摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749