CAS: 3978-80-1; Boc-Tyr-Oh

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Boc-O-苄基-L-酪氨酸置于氢气体系中,用 乙醇 作为反应溶剂,化学反应 0.75H,以93%的收率获得产物boc-L-酪氨酸
参考文献:聚氯乙烯负载的钯纳米粒子:快速氢化反应的催化剂†
标题:聚氯乙烯负载的钯纳米粒子:快速氢化反应的催化剂†
摘要:通过高效且廉价的方案制备了负载在聚氯乙烯基质(pvc-Pd 0)上的钯纳米颗粒.该催化剂已通过xrd,Sem和tem进行了表征,并证明了其在还原一系列官能团以及去除某些在肽化学中使用的常见保护基的实用性.
DOI:10.1039/c0Ob00962H

专利信息

专利号:US-7301006-B2
优先权日:2002-07-16
标 题 :Methods and materials for the synthesis of modified peptides
发明人：YOUNG TRAVIS G; KIESSLING LAURA L
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove α-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified. Preferred side-chain protecting groups are chemically distinguishable from the azide-bearing protecting group and substantially orthogonal reaction conditions can be selected such that side-chain protection of other amino acids is maintained when the azide-bearing protecting group is removed. The use of the azide-bearing protecting group of this invention for one or more hydroxy amino acids during peptide synthesis allows the selective unmasking of those azide-protected side-chain hydroxyl groups and selective modification of the hydroxyl groups that are selectively unmasked. The methods and materials herein are particularly used in synthesis of sulfated, phosphorylated and glycosylated peptides and proteins. Kits and methods of synthesizing a modified peptide or protein using the kits are also provided.

专利号:US-5026773-A
优先权日:1987-03-11
标 题 :Apparatus for a solid phase synthesis of peptide analogs
发明人：STEEL SAMUEL
权利人:STEEL SAMUEL
摘要:A novel polymeric disc, wafer or similarly shaped resin for carrying out the synthesis of peptide analogs via solid phase peptide synthesis techniques is provided. The polymeric disc or wafer of the invention may be made out of those resin materials presently used in bead form in solid phase peptide synthesis, such as, benzhydrylamine resins, Boc-aminoacyl-4-(oxymethyl)-phenyacetamidomethyl (Pam) resin, polyamide resins and chloromethyl resins. The disc or wafer of the invention should, preferably, have a thickness of 200-400 mu m and may be of any suitable length or width. A process for the synthesis of peptide analogs utilizing the polymeric disc or wafer of the present invention is also disclosed.

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:US-5746982-A
优先权日:1996-02-29
标题 :Apparatus for automated synthesis of chemical compounds
发明人：SANEII HOSSAIN; BOROOMAND MOHAMMAD R; FERRIELL MICHAEL R
权利人:ADVANCED CHEMTECH INC
摘要:Apparatus for the synthesis of chemical compounds consists of a housing having a top, front, side and rear walls surrounding and enclosing a reaction table. A track on the rear wall of the housing carries a pair of extending arms on each of which is movably mounted a vertically extendible probe for positioning at various locations over the reaction table. At least on control syringe communicates between the probe and containers for system fluids. A programmable controller is provided for control of the syringe and probes. A reaction block on the reaction table consists of a body having an upper portion and a lower portion and an upper and lower surface and a multiplicity of reaction wells for carrying out the synthesis. Each reaction well is closed at its lower end and open to the upper surface. A flushing conduit is located adjacent each of the well and is in fluid communication with the closed lower end of the reaction well. A manifold section is in fluid communication with the flushing conduit for leading fluid into and out of the body responsive to the creation of a pressure differential between the reaction well and the manifold section. The pressure in the reaction well is greater than that in the manifold section during the flushing of the well. A heating and cooling module may be attached to the reaction block for controlling the temperature of the reaction wells.

专利号:US-6376649-B1
优先权日:1998-12-18
标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives
发明人：SEMPLE JOSEPH E; LEVY ODILE E
权利人:CORVAS INT INC
摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.

专利号:US-2018265547-A1
优先权日:2014-07-18
标 题 :Z-selective olefin metathesis of peptides
发明人：MANGOLD SHANE L; GRUBBS ROBERT H
权利人:CALIFORNIA INST OF TECHN
摘要:The invention relates generally to the synthesis of modified amino acids and modified peptides in the presence of cyclometalated catalysts. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry.