N-叔丁氧羰基-3-(4-联苯基)-L-丙氨酸置于三氟乙酸体系中,用 二氯甲烷 用作溶剂,化学反应 2.0H,反应生成L-4,4'-联苯丙氨酸 参考文献:Design,Synthesis,And Bioevaluation Of Viral 3C And 3C-Like Protease Inhibitors 标题:Design,Synthesis,And Bioevaluation Of Viral 3C And 3C-Like Protease Inhibitors 摘要:A Class Of Tripeptidyl Transition State Inhibitors Containing A P1 Glutamine Surrogate,A P2 Leucine,And A P3 Arylalanines,Was Found To Potently Inhibit Norwalk Virus Replication In Enzyme And Cell Based Assays. An Array Of Warheads,Including Aldehyde,A-Ketoamide,Bisulfite Adduct,And A-Hydroxyphosphonate Transition State Mimic,Was Also Investigated. Tripeptidyls 2 And 6 Possess Antiviral Activities Against Noroviruses,Human Rhinovirus,Severe Acute Respiratory Syndrome Coronavirus,And Coronavirus 229E,Suggesting A Broad Range Of Antiviral Activities. (C) 2013 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2013.09.070
专利号:US-9139515-B2 优先权日:2011-08-19 标 题:Synthesis of R-biphenylalaninol 发明人:HERMSEN PETRUS JOHANNES; ERMANN PETER HANS; RIEBEL PETER HANS; WOLBERG MICHAEL; DE VRIES ANDREAS HENDRIKUS MARIA 权利人:HERMSEN PETRUS JOHANNES; ERMANN PETER HANS; RIEBEL PETER HANS; WOLBERG MICHAEL; DE VRIES ANDREAS HENDRIKUS MARIA; DPX HOLDINGS BV 摘要:This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The invention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.
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-2023212788-A1 优先权日:2020-03-26 标 题:New method for automated on-demand biomolecular array synthesis 发明人:ZHANG YIXIN; LIN WEILIN 权利人:UNIV DRESDEN TECH 摘要:The invention provides an amphiphilic coating for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, comprising a hydrophilic chemical structure and a lipophilic group, wherein said peptides and small molecular compounds differ from spot to spot from each other in the chemical structure, characterized in that said amphiphilic coating possesses low wettability to polar aprotic solvents used in the array synthesis; said amphiphilic coating possessing low wettability is designed that it can be converted to a coating possessing high wettability by hydrolysis of the lipophilic group; and said amphiphilic coating comprises an amino group for the reaction with an electrophilic reagent. The invention further provides a solid support comprising said amphiphilic coating and a method for method for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, wherein said planar surface of a solid support comprises said amphiphilic coating. Said method includes the enhancing of the wettability of a glass surface to organic solvents to realize automated on-demand biomolecular array synthesis comprising both, peptides and small molecular compounds. The amphiphilic surface can be switched to a hydrophilic surface, resulting in high density arrays suitable for protein- and cell-based screening.
专利号:WO-9931124-A1 优先权日:1997-12-12 标 题:Cholic acid-based scaffolds for multidimensional molecular presentation of peptides 发明人:HOEEG-JENSEN THOMAS 权利人:NOVO NORDISK AS; HOEEG JENSEN THOMAS 摘要:A solid phase method for the synthesis of a plurality of differently substituted cholic acid scaffolds with a wide variety of peptide chain, pseudo-peptide chain or peptoid chain substitutents, as leads or compounds of potential therapeutic interest. The substituted cholic acids are prepared by initial solution synthesis of a scaffold holding amino acids with 3 orthogonal protecting groups. Subsequent solid-phase synthesis provides the build-up of the target molecules, either as discretes or in mixture. The molecules may be screened on the resin or cleaved from the resin and then screened in solution. The method disclosed here provides an easy and fast access to highly diverse compounds, potential peptide mimetics and potential leads for compounds of therapeutic interest. The method is amenable to automatization.
专利号:WO-2008098280-A1 优先权日:2007-02-16 标题:Methods for the synthesis of dicarba bridges in growth hormone peptides 发明人:ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA 权利人:POLYCHIP PHARMACEUTICALS PTY; UNIV MONASH; ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA 摘要:The invention relates to peptides comprising the carboxy terminal sequence of a growth hormone or an analogue of such a peptide in which the disulfide bridge is replaced by a dicarba bridge. Compositions containing such dicarba bridged peptides and method of treating obesity in an animal such as a human comprising administration of such dicarba bridged peptides are also disclosed.
专利号:US-2024400608-A1 优先权日:2021-09-03 标题:Synthesis of bicycle toxin conjugates, and intermediates thereof 发明人:WITTY DAVID; LIMB DARREN; MIN BYOUNG JOON; HE LIWEN; SANDERS WILLIAM J; NNANABU ERNEST OBINNA 权利人:BRICYCLETX LTD 摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.
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合成参考文献
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