CAS: 952234-37-6; N-Diazoimidazole-1-Sulfonamide

上下游产品

1H-imidazole 3-(imidazole-1-sulfonyl)-1-methyl-3H-imidazol-1-ium triflate

📜咪唑置于sodium Azide,磺酰氯体系中,用 乙腈 作为反应溶剂,以60.3%的收率获得产物1H-咪唑-1-磺酰叠氮
参考文献:一种独特而快速的方法,可以有效地开发基于"点击"伪糖肽的新型蛋白质酪氨酸磷酸酶(ptp)抑制剂
标题:一种独特而快速的方法,可以有效地开发基于"点击"伪糖肽的新型蛋白质酪氨酸磷酸酶(ptp)抑制剂
摘要:蛋白质酪氨酸磷酸酶(ptp)抑制剂的开发引起了人们的极大兴趣,因为许多ptp成员与主要的人类疾病(包括自身免疫性疾病,糖尿病和癌症)紧密相关.我们在这里报告了一种独特而快速的方法,用于开发基于三唑基假糖肽的新型ptp抑制剂实体.通过使用微波加速的cu(i)催化的叠氮化物-炔烃1,3-偶极环加成反应(cuaac或"点击反应"),一系列三唑连接的丝氨酰基,苏氨酸,苯丙氨酰基和酪氨酰基1-O-葡萄糖-或半乳糖苷仅在约30分钟内就可以高产率高效合成.连续的生物学分析鉴定出这些糖肽三唑是有利的ptp1B和cdc25B抑制剂,对tcptp,Lar,Shp-1和shp-2具有选择性.确定引入的氨基酸(ser,Thr,Phe和tyr)的结构多样性和单糖支架上的差向异构体(glc或gal)均会影响相应的抑制活性和选择性.此外,已证明苄基糖支架在增强抑制剂与靶向ptp的结合亲和力中起关键作用.最终进行了对接
DOI:10.1016/j.Bmcl.2010.12.126

专利信息

专利号:US-11912647-B2
优先权日:2020-05-22
标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation
发明人：CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS
权利人:UNIV GEORGIA
摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

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-10183962-B2
优先权日:2014-02-25
标 题:Synthetic oligomers of Neisseria meningitis serogroup X and process of preparing them
发明人：GILL DAVINDER; HARALE KISHORE; CHHIKARA MANOJ KUMAR
权利人:MSD WELLCOME TRUST HILLEMAN LABORATORIES PVT LTD
摘要:The present invention relates to synthesis of novel higher oligomers and process of preparing the same. In particular the present invention relates to the chemical synthesis of oligomers of Neisseria meningitidis serogroup X (‘hereinafter Men-X), more particularly tetramer. The present invention provides Men-X capsular oligomers obtained from synthetic pathway using purified saccharides of specific chain length and provides said novel oligomers as candidates for the development of conjugate vaccine against bacterial meningitis caused due to Men-X infections.

专利号:US-10377699-B2
优先权日:2013-11-06
标 题 :Daptomycin analogues and a method for the preparation of daptomycin or a daptomycin analogue
发明人：LI XUECHEN; LAM HIU YUNG
权利人:UNIV HONG KONG
摘要:A method for the synthesis of daptomycin or a daptomycin analog is carried out on a resin to form a linear precursor followed by a serine ligation macrocyclization in solution. Daptomycin analogs can differ from daptomycin by substitution of amino acids residues and/or deletion or addition of amino acid residues. Daptomycin analogs can include a different fatty acid in the side arm of the daptomycin analog.

专利号:US-11993627-B2
优先权日:2017-07-03
标题 :Enzymatic synthesis of homogeneous chondroitin sulfate oligosaccharides
发明人：LIU JIAN; LI JINE; SU GUOWEI
权利人:UNIV NORTH CAROLINA CHAPEL HILL
摘要:Methods of synthesizing chondroitin sulfate oligosaccharides are provided. Enzymatic schematic approaches to synthesizing structurally defined homogenous chondroitin sulfate oligosaccharides at high yields are provided. Synthetic chondroitin sulfate oligosaccharides ranging from 3-mers to 15-mers are provided.

专利号:US-2024309035-A1
优先权日:2017-07-03
标题 :Enzymatic synthesis of homogeneous chondroitin sulfate oligosaccharides