CAS: 3984-14-3; N,N-Dimethylsulfamide

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二甲胺基磺酰氯置于ammonium Hydroxide体系中,用37%的收率获得产物n,N-二甲基磺酰胺
参考文献:光化学介导的镍催化合成 N-(杂)芳基磺酰胺.
标题:光化学介导的镍催化合成 N-(杂)芳基磺酰胺.
摘要:描述了磺酰胺与芳基溴进行 N-芳基化的一般方法.该方案利用双催化系统,以[ir(Ppy)2(Dtbbpy)]Pf6作为光敏剂,Nibr2.glyme作为预催化剂,以及1,8-二氮杂双环(5.4.0)Undec-7-Ene (Dbu))作为基础,并在可见光照射下在室温下进行.使用这些策略,芳基硼酸酯和芳基氯可以在反应中不受影响地进行.所开发的反应有效地参与简单的溴代芳烃和伯磺酰胺,产率在 66% 和定量之间.对于更具挑战性的底物,例如仲磺酰胺,反应效率被记录下来.因此,这些方法补充了已知的用于磺酰胺n-芳基化的buchwald-Hartwig偶联方法.
DOI:10.1021/acs.Joc.0C00139

专利信息

专利号:US-10266565-B2
优先权日:2011-04-12
标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN
权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.

专利号:WO-2017082924-A1
优先权日:2015-11-13
标题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE TERRENCE R JR; HYMEL DAVID
权利人:THE US SECRETARY DEPT OF HEALTH & HUMAN SERVICES
摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

专利号:US-10905769-B2
优先权日:2015-11-13
标 题:Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE JR TERRENCE R; HYMEL DAVID T; TSUJI KOHEI
权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. Exemplary compounds of the description include macrocyclic peptidomimetics with high affinity and selectivity for polo-like kinases, which may provide the basis for a new genre of anticancer therapeutics. Other exemplary compounds of the description include bi-valent compounds with that bind to polo-like kinases through both kinase domain and polo-box domain simultaneously by incorporating additional moieties that target Plk1 kinase domain, which significantly enhances affinitity relative and may provide the basis for a new genre of anticancer therapeutics. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

专利号:US-2024368075-A1
优先权日:2021-07-02
标题 :Synthesis of N,N-Dialkyl, -Dialkenyl, -Dialkynyl, and Related Cyclics, Sulfamoyl Fluoride Compounds Using Hydrogen Fluoride
发明人：SINGH RAJENDRA P; HU QICHAO
权利人:SES HOLDINGS PTE LTD
摘要:Methods of producing N,N-dimethyl sulfamoyl fluoride and related derivatives of the formula F—S(O)2—NR2 (I) by contacting a sulfamoyl nonfluorohalide compound of the formula X—S(O)2—NR2 (II) with anhydrous hydrogen fluoride under conditions sufficient to produce the N,N-dimethyl sulfamoyl fluoride or derivative thereof of Formula I, wherein R in each of Formulas I and II is, independently, a linear or branched alkyl, alkenyl, or alkynyl group containing 1 to 12 carbon atoms, the Rs can be joined to form a cyclic amine with the N, and X is any one of chlorine, bromine, and iodine.

专利号:US-2023322661-A1
优先权日:2020-08-21
标题 :Synthesis of N,N-Branched Sulfamoyl Fluoride Compounds Using Bismuth Trifluoride
发明人：SINGH RAJENDRA P; HU QICHAO; SHEIMAN JOHNATHAN
权利人:SES HOLDINGS PTE LTD
摘要:Methods of producing N,N-branched sulfamoyl fluoride compounds of the formula F-S(O) 2 -NR 2 by contacting bismuth trifluoride with an N,N-branched sulfamoyl nonfluorohalide compound of the formula X-SO 2 NR 2 , wherein X=chlorine (Cl), bromine (Br), or iodine (I), and each R is, independently, a linear or branched alkyl, fluoroalkyl, alkenyl, fluoroalkenyl, alkynyl, or fluoroalkynyl with 1 to 12 carbon atoms, to fluorinate the N,N-branched sulfamoyl nonfluorohalide compound. This is a non-aqueous method, the purity of product is very high, and the desired product can be isolated in quantitative yield. The N,N-branched sulfamoyl fluoride compounds so produced are useful in various applications including as electrolyte solvents and additives in electrochemical devices, such as lithium batteries and capacitors, and in biological fields, among others.

专利号:US-7842834-B2
优先权日:2005-07-21
标 题:Process for the synthesis of sulfonyl halides and sulfonamides from sulfonic acid salts
发明人：MICHALAK RONALD S; HELOM JEAN L; ZELDIS JOSEPH
权利人:WYETH LLC
摘要:The present invention provides synthetic processes for the preparation of sulfonyl halides of Formula Ar—(R) z —SO 2 —X and sulfonamides of Formula Ar—(R) z —SO 2 —NR 4 R 5 , where the constituent variables are as defined herein, that are useful as intermediates in the preparation of pharmaceuticals.