CAS: 2158-14-7; 4-(Acetylamino)Benzenesulfonyl Azide

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CAS号121-60-8 对乙酰氨基苯磺酰氯 | CAS号121-62-0 4-乙酰氨基苯磺酸 | CAS号14860-69-6 4-amino-N-diazo... | CAS号90965-06-3 (1-重氮基-2-氧代丙基)膦酸二甲酯 | CAS号2158-18-1 N-[4-[(2,5-dime... | CAS号121-61-9 4-乙酰氨基苯磺酰胺 | CAS号27491-70-9 P-(重氮甲基)磷酸二甲酯 | CAS号758692-47-6 2-(4-溴苯基)-2-重氮基乙酸乙酯 | CAS号132316-71-3 2-diazonio-1-(3... | CAS号1422277-71-1 (E)-N1,N1-diiso... | CAS号1422277-72-2 N1,N1-diethyl-N...

对乙酰胺基苯磺酰氯置于sodium Azide,四丁基溴化铵体系中,用 二氯甲烷,水 用作溶剂,化学反应 16.0H,以61%的收率获得4-乙酰氨基苯磺酰叠氮
参考文献:由天然羊毛硫氨酸abc片段和交叉修饰的合成de片段组成的具有生物活性的乳链菌肽杂种的半合成
标题:由天然羊毛硫氨酸abc片段和交叉修饰的合成de片段组成的具有生物活性的乳链菌肽杂种的半合成
摘要:抗菌肽乳链菌肽是一种有前途的模板,可用于设计新型的基于肽的抗生素以改善其类似药物的特性.在该方向上的第一步代表了杂合乳链菌肽衍生物的合成,其中包含天然乳链菌肽abc部分和合成的交叉订正de环片段,在此进行了描述.评价了新合成的乳链菌肽衍生物的生物活性,以便比较含有模拟物的合成de-环和含有乳链菌肽的天然羊毛硫氨酸桥连的de-环的生物活性.天然乳链菌肽abc-环系统是通过胰凝乳蛋白酶消化全长乳链菌肽获得的,随后在c末端的羧酸根上被两个不同的氨基炔基部分官能化.下一个,乳酸链球菌素杂种是使用cu(i)催化的叠氮化物炔烃环加成" Click"化学方法,通过将abc炔烃与n末端叠氮基官能化的双氨基甲酸酯-De环模拟物化学选择性连接而成功制备的.新合成的化合物作为有效的脂质ii粘合剂具有活性,并在生长抑制试验中保留了抗菌活性.但是,未观测到孔的形成,可能是由于"订书钉"与母体硫化物相比的特性不同,或
Doi:10.1016/j.Bmc.2014.07.046

专利信息

专利号:WO-9740025-A1
优先权日:1996-04-19
标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA
摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:WO-2023039068-A1
优先权日:2021-09-08
标题:Compositions and methods for synthesis of peptide nucleic acid intermediates
发明人：COULL JAMES M; GILDEA BRIAN D
权利人:NEUBASE THERAPEUTICS INC
摘要:The present disclosure provides intermediates for the synthesis of peptide nucleic acid (PNA) backbones and monomers, such as cyclic intermediates, and methods of making the same.

专利号:US-10829792-B2
优先权日:2017-03-21
标 题 :Biocatalytic synthesis of strained carbocycles
发明人：CHEN KAI; HUANG XIONGYI; KAN S B JENNIFER
权利人:CALIFORNIA INST OF TECHN
摘要:Provided herein are methods for producing products containing strained carbocycles, such as cyclopropene moieties and/or bicyclobutane moieties. The methods include combining an alkyne and a carbene precursor in the presence of a heme protein, e.g., a cytochrome P450, under conditions sufficient to form the strained carbocycle. Reaction mixtures for producing strained carbocycles are also described, as well as whole-cell catalysts comprising heme proteins and variants thereof for forming cyclopropenes, bicyclobutanes, and related products.

专利号:US-8853132-B2
优先权日:2008-11-27
标题 :Directed synthesis of oligophosphoramidate stereoisomers
发明人：HEINDL DIETER; KESSLER DIRK; ROESLER ANGELIKA; SEIDEL CHRISTOPH; THUER WILMA
权利人:ROCHE DIAGNOSTICS OPERATIONS
摘要:The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.

专利号:US-2024239805-A1
优先权日:2022-12-16
标 题:Aza-yang cyclization-buchner aromatic ring expansion: collective synthesis of cycloheptatriene-containing azetidine lactones
发明人：SINGH MANVENDRA PAL; BOSKOVIC ZARKO; GASKINS BRYCE
权利人:UNIV KANSAS
摘要:The present disclosure is directed to a compound of Formula I, Formula II, Formula III, Formula IV, or Formula Vor a pharmaceutically acceptable salt and/or solvate thereof.

专利号:US-2010022541-A1
优先权日:2006-09-25
标题:Chemical inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
发明人：ESCAICH SONIA; DENIS ALEXIS; MOREAU FRANCOIS; GERUSZ VINCENT; DESROY NICOLAS
权利人:ESCAICH SONIA; DENIS ALEXIS; MOREAU FRANCOIS; GERUSZ VINCENT; DESROY NICOLAS
摘要:The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR 1 , C1-C10 alkyl-NR 1 R 1 , alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO 2 R 1 , NR 1 R 1 , NR 1 C(O)R 1 , C(O)NR 1 R 1 , NR 1 C(S)R 1 , C(S)NR 1 R 1 , SO 2 NR 1 R 1 , SO 2 R 1 , NR 1 SO 2 R 1 , NR 1 C(O)NR 1 R 1 , NR 1 C(O)OR 1 , NR 1 C(S)NR 1 R 1 , NR 1 C(S)OR 1 , R 1 Câ•?NOR 1 , C(O)R 1 , aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B 1 , B 2 , B 3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B 4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined aboe.