合成目标产物 6-Methyluracil 主要起始原料 Ethyl Acetoacetate And Urea
(文献来源)合成步骤主要原料 Ethyl Acetoacetate 和 Urea
4-甲基嘧啶置于agrobacterium Sp. Dsm 6136体系中,化学反应 30.0H,以78%的收率获得产物6-甲基尿嘧啶 参考文献:Fungal And Bacterial Regioselective Hydroxylation Of Pyrimidine Heterocycles 标题:Fungal And Bacterial Regioselective Hydroxylation Of Pyrimidine Heterocycles 摘要:The Bacterium Rhodococcus Erythropolis Is Employed To Hydroxylate The Anxiolytic Lesopitron,And This Bacterium,Together With Agrobacterium Sp. And The Fungus Beauveria Bassiana,Are Used To Extend The Field Of Hydroxylation Of Heteroaromatic Compounds To A Series Of Unexplored Pyrimidines. Of All The Substrates Investigated,Only The Carbamate 11A Is Regioselectively Hydroxylated By B. Bassiana At The C-5 Position Of The Pyrimidine Ring; In Contrast,The Bacteria Are Able To Regioselectively Oxidize,When Free,The C-2 And/or C-4 Positions Of The Pyrimidine Moiety Of All The Substrates 1A-12A,Up To A Maximum Of Two Oxidations. (C) 1997 Elsevier Science Ltd. DOI:10.1016/s0040-4020(97)00301-3
专利信息
专利号:US-11028057-B2 优先权日:2018-02-28 标题:Process for the synthesis of 6-chloromethyluracil 发明人:MORANA FABIO; GOBBATO STEFANO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:The invention relates to a process for the synthesis of 6-chloromethyluracil (6-(chloromethyl)pyrimidin-2,4(1H,3H)-dione) from ethyl 4-chloroacetoacetate and S-methylisothiourea hemisulfate via isolation of the novel intermediate 6-(chloromethyl)-6-hydroxy-2-(methylthio)-5,6-dihydropyrimidin-4(1H)-one, and its subsequent treatment with aqueous sulfuric acid. Formula (I).
专利号:US-10882884-B2 优先权日:2016-05-18 标题:Stereoselective synthesis of phosphorothioate oligoribonucleotides 发明人:HALL JONATHAN; LI MEILING 权利人:ETH ZUERICH 摘要:The present invention relates to chiral phosphoramidites represented by formula (Ia) or formula (Ib) n n n n n n n n n n n n as novel monomers for the synthesis of stereodefined phosphorothioate MOE oligonucleotides. Furthermore, the present invention relates to a method for synthesizing stereodefined phosphorothioate MOE oligonucleotides using said novel chiral phosphoramidites.
专利号:WO-0119801-A1 优先权日:1999-09-16 标题 :Bioactive substance containing derivatives of 2-amino-6-aryloxypyrimidines and intermediary products of synthesis thereof 发明人:ASHKINAZI RIMMA ILIINICHNA; GANINA MARIYA BORISOVNA; STUDENTSOV EVGENY PAVLOVICH 权利人:ASHKINAZI RIMMA ILIINICHNA; GANINA MARIYA BORISOVNA; STUDENTSOV EVGENY PAVLOVICH 摘要:The invention relates to novel bioactive compounds of the family of pyrimidines and to intermediary products, of the synthesis of such compounds. The novel compounds have a strong antimicrobial activity (especially in respect to a strain of mycobacterium resisting to the existing drugs) and a strong antiviral activity in addition to a strong immunostimulating (interferonogenic) activity while at the same time having a low toxicity level. The derivatives of 2-amino-6-aryloxypyrimidines and intermediary products of the synthesis of such compounds correspond to the following general formula: (formula I) where R1 is preferably selected from a group containing amino, C1-C4 monoalkylamino, dialkylamino, carboxyalkylamino, arylamino, heterylamino groups; R2 represents halogen atoms or an alkyl, hydroxyl, amino or alkoxy group; R3 represents hydrogen or halogen atoms; R4 represents halogen atoms, aryloxy groups with functional X substituents in ortho-, meta- and para positions of the aryl fragment, whereby X substituents are halogen atoms, alkyls C1-C4, cycloalkyl, alkenyl, alkoxy and nitro groups. The invention also relates to the pharmaceutically acceptable salts thereof.
专利号:EP-0799313-A2 优先权日:1994-12-13 标 题 :Method and reagent for treatment of arthritic conditions, induction of graft tolerance and reversal of immune responses 发明人:BEIGELMAN LEONID; STINCHCOMB DANIEL T; JARVIS THALE; DRAPER KENNETH; PAVCO PAMELA; MCSWIGGEN JAMES; GUSTOFSON JOHN; USMAN NASSIM; WINCOTT FRANCINE; MATULIC-ADAMIC JASENKA; KARPEISKY ALEXANDER; THOMPSON JAMES D; MODAK ANIL; BURGIN ALEX 权利人:RIBOZYME PHARM INC 摘要:An enzymatic nucleic acid molecule which cleaves RNA associated with development or maintenance of an arthritic condition, induction of graft tolerance or reversal of an immune response. In particular, the ribozyme sequences are directed to an mRNA encoding B7-1, B7-2, B7-3, CD40 and/or stromelysin. Also provided are ribozymes where the uracil in positions 4 and/or 7 are substituted, as well as methods for the synthesis of 2'-alkylnucleotides, 2'-O-alkylthioalkyl, or 2'-alkylthioalkylnucleotides. The application further describes a method for diprotection of RNA with aqueous ethylamine, a method for synthesis of a basic ribonucleoside mimetics, and transcription units comprising an RNA polymerase II promoter, a U6 small nuclear promoter, or an adenovirus VA1 promoter system.
专利号:US-2006115536-A1 优先权日:2004-11-12 标 题 :Glycerin based synthesis of silver nanoparticles and nanowires 发明人:YACAMAN MIGUEL J; ELECHIGUERRA JOSE L; BURT JUSTIN L; MORONES JOSE R; LOPEZ LETICIA L 权利人:UNIV TEXAS 摘要:The present invention includes compositions and methods for the production of noble metal nanoparticles and nanowires conjugated to polyols or polymers. The present invention allows the incorporation of noble metal nanoparticles to a wide range of products such as body care products to exploit the biocidal properties of silver nanoparticles against bacteria, viruses and fungi.
专利号:US-11840519-B2 优先权日:2019-09-03 标 题 :Process for the synthesis of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2.6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process 发明人:LENNA ROBERTO; FASANA ANDREA; ORTIZ JERRY 权利人:IND CHIMICA SRL 摘要:The present invention to a process for the preparation of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]-amino]-butanoic acid, compound also known as Elagolix sodium salt, having the formula (I) reported below:
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