合成目标产物 Thioanisole 主要起始原料 Thiophenol And Iodomethane
(文献来源)合成步骤主要原料 Thiophenol 和 Iodomethane
1,4-二氯苯置于bis(Triphenylphosphine)Nickel(II) Chloride体系中,用 苯 用作溶剂,化学反应 5.0H,反应生成茴香硫醚 参考文献:Selective Mono-Arylation And-Alkylation Of Chlorophenyl Alkyl Sulfides By Nickel Catalysed Cross-Coupling With Grignard Reagents 标题:Selective Mono-Arylation And-Alkylation Of Chlorophenyl Alkyl Sulfides By Nickel Catalysed Cross-Coupling With Grignard Reagents 摘要: Doi:10.1016/s0040-4039(00)85672-5
专利信息
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-2003125243-A1 优先权日:2000-07-20 标题:Synthesis of cyclic peptides 发明人:LIU JUN; DAI XUEDONG; SU ZHUANG 摘要:The cyclic pentapeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys-) is a highly potent and selective inhibitor for the α v β 3 integrin. A related compound, cyclo(-Arg-Gly-Asp-D-Phe-Val-), is a promising anticancer drug candidate; it has been found to inhibit angiogenesis and induce apoptosis in vascular cells. We have developed a synthesis of arginine containing cyclic peptides using the cyclizcation reagent 1-propanephosphonic acid cyclic anhydride (T3P) and the guanidine protecting group, 2,2,5,7,8-pentamethylchroman-6-sulfonyl (Pbf). This improved synthesis is environmentally friendly and is generally applicable to the synthesis of other cyclic peptides.
专利号:US-7956011-B2 优先权日:2005-05-04 标题:Materials and methods for the photodirected synthesis of oligonucleotide arrays 发明人:SERAFINOWSKI PAWEL JERZY; GARLAND PETER BRYAN 权利人:CANCER RES INST ROYAL 摘要:Materials and methods for photodirected synthesis of oligonucleotide arrays on a solid substrate by photodirected synthesis are disclosed which employ a film formed from (i) a photoacid generator that on photolysis generates acid that is capable of directly removing the protecting group of the linker molecules or oligonucleotides and (ii) a polymer substantially lacking electronegative heteroatoms that are capable of hydrogen bonding with photogenerated acid. Methods of synthesizing an oligomer arrays are also described that use a film that restricts diffusion of reactants and products on the substrate during synthesis of the array and which includes a precursor of a deprotecting reagent. The method involves removing one or more of the non-required products of the deprotection reaction from the reactive array elements at which they are produced during the reaction, in order to displace the deprotection reaction towards completion.
专利号:US-2023242581-A1 优先权日:2020-06-17 标题:Synthesis of a guanylate cyclase agonist by fragments based approach 发明人:SAMBASIVAM GANESH; KASTURCHAND GODHA ATUL; VENKATA BHAGYARAJ ARETI; ANNADURAI SATHYA; VEERANJANEYULU AVULA; VASANTRAO GADAKH AMOL; S JADHAV DIPAK 权利人:ANTHEM BIOSCIENCES PRIVATE LTD 摘要:The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.
专利号:WO-9817677-A1 优先权日:1996-10-24 标 题 :Improvements in solid-phase synthesis of peptides and related compounds 发明人:ENGLEBRETSEN DARREN 权利人:UNIV QUEENSLAND; ENGLEBRETSEN DARREN 摘要:The invention relates to spacers for use in solid-phase synthesis of peptides and peptide-related compounds, in which a spacer construct is used to ensure that the target peptide or peptide-related compound is at a distance equivalent to at least 5-15 amino acids from the solid support. Constructs of the invention are particularly applicable to the synthesis of strongly hydrophobic peptide, which are otherwise difficult, if not impossible to purify and analyse. The constructs and methods of the invention are also applicable to synthesis of peptide nucleic acids.
专利号:US-2012215002-A1 优先权日:2009-10-09 标 题:Synthesis of optically active intermediate for the preparation of montelukast 发明人:LEFORT LAURENT 权利人:LEFORT LAURENT 摘要:The present invention relates to the synthesis of optically active alcohols by means of enantioselective hydrogenation of ketones in biphasic systems. In particular the present invention relates to the synthesis of an optically active alcohol of general formula (1).
[参考文献]: B Frohm, Et Al. A Peptide From Human Semenogelin I Self-Assembles Into A Ph-Responsive Hydrogel. Soft Matter. 2015 Jan 14;11(2):414-21. [参考文献]: Chao Zhao, Et Al. Quantification Of Plasma Hiv Rna Using Chemically Engineered Peptide Nucleic Acids. Nat Commun. 2014 Oct 6:5:5079. [参考文献]: Giulia Caron, Et Al. Calculating Virtual Log P In The Alkane/water System (Log P(N)(Alk)) And Its Derived Parameters Deltalog P(N)(Oct-Alk) And Log D(Ph)(Alk). J Med Chem. 2005 May 5;48(9):3269-79. [参考文献]: Hyo-Eon Jin, Et Al. Selective And Sensitive Sensing Of Flame Retardant Chemicals Through Phage Display Discovered Recognition Peptide. Nano Lett. 2015 Nov 11;15(11):7697-703. [参考文献]: Jisheng Zhang, Et Al. Redox Inactive Metal Ion Triggered N-Dealkylation By An Iron Catalyst With Dioxygen Activation: A Lesson From Lipoxygenases. Dalton Trans. 2015 Jun 7;44(21):9847-59.
合成参考文献
参考文献:10.1007/978-1-61779-188-8_4 摘要:Crombez L, Morris MC, Heitz F, Divita G. A non-covalent peptide-based strategy for ex vivo and in vivo oligonucleotide delivery. Methods Mol Biol. 2011;764():59–73. doi: 10.1007/978-1-61779-188-8_4.