CAS: 7461-50-9; 2-Chloropyrimidin-4-Amine

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CAS号3934-20-1 2,4-二氯嘧啶 | CAS号71-30-7 胞嘧啶 | CAS号7664-41-7 氨 | CAS号3289-47-2 4-氨基-2-甲氧基嘧啶 | CAS号71-30-7 胞嘧啶 | CAS号245321-46-4 4-氨基嘧啶-2-甲腈 | CAS号63286-28-2 2-氯-3-肼基吡嗪 | CAS号57005-71-7 2-(4-甲基-1-哌嗪)-4-嘧啶胺 | CAS号33630-25-0 2-苯基嘧啶-4-胺 | CAS号221050-88-0 2-氯-4-(4-B°C-1-... | CAS号61310-29-0 2-(4-吡啶基)-4-氨基嘧啶

2,4-二氯嘧啶置于ammonium Hydroxide体系中,用 水 作为反应溶剂,以40%的收率获得产物4-氨基-2-氯嘧啶
参考文献:吡咯盐对氨基杂环的选择性功能化
标题:吡咯盐对氨基杂环的选择性功能化
摘要:提出了使用四氟硼酸吡啶鎓试剂(pyry-Bf 4)对氨基杂环进行官能化的方法.该试剂可与多种杂环胺有效地缩合,并为亲核芳香族取代反应准备c-N键.本文公开了用于形成co,Cn,Cs或cs 2 R键的60多个例子.与通过重氮化和多烷基化进行cn活化相反,该方法的特点是条件温和且对官能团的耐受力强.除小分子衍生化外,Pyry-Bf 4还允许以后期方式引入官能团,以提供高度官能化的结构.
DOI:10.1002/anie.201806271

专利信息

专利号:US-9574189-B2
优先权日:2005-12-01
标题:Enzymatic encoding methods for efficient synthesis of large libraries
发明人：FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK
权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS
摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).

专利号:US-7122670-B2
优先权日:2003-09-05
标题:Selective synthesis of CF3-substituted pyrimidines
发明人：KATH JOHN CHARLES; RICHTER DANIEL TYLER; LUZZIO MICHAEL JOSEPH
权利人:PFIZER
摘要:The present invention relates to a method of making a compound of the formula n nwherein X 1 , X 2 and R 3 —R 4 are as defined herein. The method includes reacting a compound of the formulan n nwith an amine of formula 3 (HNR 3 R 4 ) in the presence of a Lewis Acid and a non-nucleophilic base. The 2,4-diamino pyrimidine moiety is a common component in a variety of biologically active drug-like molecules and pyrimidine derivatives have been found to be useful in the treatment of abnormal cell growth, such as cancer, in mammals.

专利号:US-8933227-B2
优先权日:2009-08-14
标题 :Selective synthesis of functionalized pyrimidines
发明人：LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN
权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT
摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.

专利号:US-11225655-B2
优先权日:2010-04-16
标题:Bi-functional complexes and methods for making and using such complexes
发明人：GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK
权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS
摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

专利号:WO-2019013789-A1
优先权日:2017-07-12
标 题 :ANTIMICROBIAL COMPOUNDS
发明人：REDDY HARIPRASADA R KANNA; SEBAHAR PAUL R; SERRANO CATHERINE M; LOOPER RYAN E
权利人:CURZA GLOBAL LLC; THE UNIV OF UTAH RESEARCH FOUNDATION
摘要:The invention relates to compounds of formula I or their pharmaceutically acceptable salts. The compounds of formula I are antimicrobial agents which inhibit, for example, Mycobacterium tuberculosis (Mtb) H37Ra. The compounds of formula I also have anti-tuberculous activity, exhibit limited cytotoxicity and inhibit protein synthesis. The invention also relates to methods of making compounds of formula I, as well as methods of using compounds of formula I for the treatment of bacterial infections, particularly tuberculosis.

专利号:US-11702652-B2
优先权日:2005-12-01
标题:Enzymatic encoding methods for efficient synthesis of large libraries