专利号:US-12006540-B2 优先权日:2015-09-28 标题:Synthesis of novel disulfide linker based nucleotides as reversible terminators for DNA sequencing by synthesis 发明人:JU JINGYUE; LI XIAOXU; CHEN XIN; LI ZENGMIN; KUMAR SHIV; SHI SHUNDI; GUO CHENG; REN JIANYI; HSIEH MIN-KANG; CHIEN MINCHEN; TAO CHUANJUAN; ERTURK ECE; KALACHIKOV SERGEY; RUSSO JAMES J 权利人:UNIV COLUMBIA 摘要:Disclosed herein, inter alia, are compounds, compositions, and methods of use thereof in the sequencing of a nucleic acid.
专利号:US-4424159-A 优先权日:1978-05-26 标 题:Process for the synthesis of the hydroxyacetyl side-chain of steroids of the pregnane type, novel 21-hydroxy-20-oxo-17α-pregnane compounds and pharmaceutical preparations containing them 发明人:BIOLLAZ MICHEL 权利人:CIBA GEIGY CORP 摘要:The present invention relates to a novel general process for synthesizing a α- or β-oriented hydroxyacetyl side chain of steroids of the pregnane type, which comprises treating a corresponding steroid carbaldehyde in succession with formaldehyde dimethylmercaptal-S-oxide in the form of an alkali metal salt thereof, and with a strongly acid hydrolysing agent. n Preferred final products are compounds of the formula ##STR1## wherein n is 1 or 2, R 2 represents methyl or difluoromethyl, and R 1 represents hydroxymethyl, methoxymethyl, acetoxymethyl or hydrogen, and, if n is 2 and/or R 2 is difluoromethyl, R 1 also represents methyl. These compounds act as agonists or antagonists of natural steroid hormones. The antigestagenic 19,21-dihydroxy-17α-pregn-4-ene-3,20-dione and its 6,7-dehydro derivatives and diacetates are of particular interest.
专利号:US-5808071-A 优先权日:1996-09-27 标题 :Pictet-Spengler reaction for the synthesis of tetrahydroisoquinolines and related heterocyclic compounds 发明人:WATSON TIMOTHY JAMES-NORMAN 权利人:HOECHST MARION ROUSSELL INC 摘要:A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of a suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.
专利号:EP-0929527-B1 优先权日:1996-09-27 标题 :Pictet-spengler reaction for the synthesis of tetrahydroisoquinolines and related heterocyclic compounds 发明人:WATSON TIMOTHY JAMES-NORMAN 权利人:AVENTIS PHARMA INC 摘要:A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.
专利号:US-8030496-B2 优先权日:2005-02-17 标 题:Intermediate compound for synthesis of viridiofungin a derivative 发明人:KATO TATSUYA; KIMURA NOBUAKI; MIZUTANI AKEMI; MAKINO TOSHIHIKO; KAWASAKI KENICHI; FUKUDA HIROSHI; KOMIYAMA SUSUMU; TSUKUDA TAKUO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. n A compound represented by the formula (1-8): n n n n n n n n n n n n wherein Y represents a group represented by the following formula: n n n n n n n n n n n n n n n n Q represents a protected carbonyl group; D represents —(CH 2 ) m —R′, etc.; and n represents an integer of 0 to 10.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
参考标题:An Asymmetric Approach To 2-Deoxynucleosides Via Organosulfur Building Blocks As Chemical Chameleons 作者:Barry M. Trost,Christoph Nübling |发布日期:1990.7 摘要:Asymmetric Synthesis Of 6-N-Benzoyl-5'-O-Benzyl-2'-Deoxyadenosine And Its A Anomer From Non-Carbohydrate Building Blocks Is Achieved In 7 Steps. The Sequence Builds The Basic Structures Using Bis(Methylthio)Methane And Methylthiomethyl Phenyl Sulfone As Both Nucleophilic And Electrophilic Building Blocks, A Feature That Suggests Their Behavior As Chemical Chameleons. The Asymmetric Induction Is Achieved
合成参考文献
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