CAS: 934-34-9; Benzothiazolone

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苯并噻唑置于氧气,三氟乙酸酐,Copper Dichloride体系中,用 乙腈 作为反应溶剂,以70 %的收率获得产物2-羟基苯并噻唑
参考文献:Copper‐catalyzed Stepwise Aerobic Oxidation/n‐arylation From Benzothiazole
标题:Copper‐catalyzed Stepwise Aerobic Oxidation/n‐arylation From Benzothiazole
摘要:摘要 我们在此报告一种 3-芳基苯并噻唑啉-2-酮化合物的高效合成方法.首先,在 Cucl2 和三氟乙酸酐存在下,取代的苯并噻唑可以顺利氧化为苯并噻唑啉-2-酮衍生物.其次,在 Cu2S 催化下,苯并噻唑啉-2-酮与芳基硼酸发生 N-芳基化反应,反应生成一系列新型 3-芳基苯并噻唑啉-2-酮衍生物.该方法对多种底物都有很好的产率,并显示出与官能团的非常好兼容性.3-芳基苯并噻唑啉-2-酮的衍生化进一步说明了该骨架的实用性.机理研究表明,苯并噻唑的氧化可能经历了一个自由基反应过程.
DOI:10.1002/ejoc.202301108

专利信息

专利号:US-6683189-B1
优先权日:1996-02-26
标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
发明人：DERVAN PETER B; BAIRD ELDON
权利人:CALIFORNIA INST OF TECHN
摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

专利号:WO-2010103857-A1
优先权日:2009-03-12
标 题 :Method for solid-phase synthesis of glycopeptide using silicon-containing protecting group and synthesis device
发明人：NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN
权利人:UNIV HOKKAIDO NAT UNIV CORP; NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN
摘要:Disclosed are a novel method for the synthesis of a glycopeptide by which glycopeptides of various types can be deprotected and excised from a resin, each under weakly acidic to weakly basic conditions, without causing the problems of the epimerization of an amino acid at the a-position and the ß-elimination of a sugar residue; a synthesis device therefor; and a synthesis intermediate to be used in synthesizing a glycopeptide. Specifically disclosed are a method for the solid-phase synthesis of a glycopeptide which comprises a step for obtaining a glycopeptide derivative wherein the N-terminus is protected, the C-terminus is immobilized to a solid phase via a silicon linker, and a reactive group carried by a sugar residue and a reactive group carried by an amino acid side chain constituting a peptide are protected by silicon-containing groups, and a step for obtaining the glycopeptide by deprotecting said glycopeptide derivative and releasing the same from the solid phase by treating the glycopeptide derivative with an agent for removing the silicon-containing groups and the silicon linker; a synthesis intermediate to be used in the step for obtaining the glycopeptide derivative in the aforesaid method; and a device for the solid-phase synthesis of a glycopeptide.

专利号:US-2008287649-A1
优先权日:2006-12-29
标 题 :Methods for the synthesis of cyclic peptides
发明人：CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R
权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R
摘要:Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:WO-9707129-A1
优先权日:1995-08-18
标题 :Solution synthesis of peripheral acting analgesic opioid tetrapeptides
发明人：RINALDI NICHOLAS
权利人:IAF BIOCHEM INT; RINALDI NICHOLAS
摘要:This invention provides a bulk scale process for the solution synthesis of enantiomerically pure peripherally acting analgesic opioid tetrapeptides corresponding to formula (I): Tyr-(D)R1-R2-R3-NH2, where R1 is Ala or Arg; R2 is Phe or Phe(p-F); and R3 is Phe or Phe(p-F). A new and unique multi-step process is disclosed comprising the joining of two dipeptides using standard solution phase synthesis techniques, but adjusting the individual factors (e.g., solvents, activating agents, neutralizing agents etc.), to minimize racemization of the second amino acid. Tremendous cost efficiencies are achieved due to elimination of traditional sequential blocking-deblocking cycles and multiple chromatographic purification steps, which also enables these simple kilogram quantity methods to be scaled up to commercial production.

专利号:EP-1246837-B1
优先权日:2000-01-11
标 题:Oligomers of nonpeptide restricted mimetics of dipeptides or tripeptides and the use thereof in the synthesis of synthetic proteins and polypeptides
发明人：AMBLARD MURIEL; MARTINEZ JEAN; BERGE GILBERT
权利人:CENTRE NAT RECH SCIENT
摘要:The invention relates to nonpeptide oligomers of amino acids. The oligomers comprise -(NR'-A-CO)-O- units which represent a nonpeptide, restricted-mimetic inducer of the beta turn in a dipeptide or tripeptide fragment. Said oligomers may be produced by peptide synthesis techniques, whether in solution or in the solid phase, and can be used in the synthesis of synthetic proteins or polypeptides, in which the peptide fragment(s) (is) are identical to those of the corresponding natural protein or polypeptide and whose structural fragment(s) comprise(s) a fragment of an oligomer according to the invention.