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参考文献:Cyrene:一种用于芳基碘化物 Mizoroki-heck 反应的生物基溶剂
标题:Cyrene:一种用于芳基碘化物 Mizoroki-heck 反应的生物基溶剂
摘要:开发更绿色和更可持续的方法,以及使现有协议适应更环保的程序,已成为有机合成的关键.引入和利用更环保的溶剂是一种非常有前途的替代品,特别是当它们可以在已知和广泛使用的有机反应中替代有毒有机溶剂时.cyrene 似乎是许多有机反应的极佳替代溶剂.在这项工作中,描述了一种新的,更环保,更经济的 Mizoroki-heck 反应方案的开发,使用 Cyrene 作为绿色溶剂,Pd/c 作为钯催化剂源.展示了芳基碘与丙烯酰胺,丙烯酸酯,丙烯酸,丙烯腈和苯乙烯偶联的广泛底物范围.cyrene 的可回收性和最终产品中钯的浸出进行了检查,以提高该协议的工业适用性.此外,还报道了天然产物哌洛汀 A 的合成.
DOI:10.1039/d2Ob02012B
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专利信息
专利号:WO-2011048029-A1
优先权日:2009-10-20
标题:Cyclic peptide synthesis
发明人:HUSBYN METTE
权利人:GE HEALTHCARE AS; HUSBYN METTE
摘要:The present invention relates to an improved method of synthesis of cyclic peptides comprising 2 or more disulfide bonds, using the reagent bispyridyl disulfide. Also disclosed is the application of the method to specific cMet-targeting peptides.
专利号:US-6346632-B1
优先权日:1990-05-17
标题 :Process for the preparation of intermediates useful for the synthesis for benzothiazepines
发明人:GHIROTTO LUCA; SERVI STEFANO; FUGANTI CLAUDIO; GENTILE ANGELO; GIORDANO CLAUDIO
权利人:ZAMBON SPA
摘要:A process for the preparation of the compounds of formula n (wherein R has the meanings reported in the specification) by enzymatic transesterification of enantiomeric mixtures is described. n These compounds are intermediates useful in the synthesis of Diltiazem.
专利号:US-7566697-B2
优先权日:2002-06-10
标题 :Carboxy protection strategies for acidic C-terminal amino acids in chemical ligation of oligopeptides
发明人:BOTTI PAOLO; VILLAIN MATTEO; MANGANIELLO SONIA; GAERTNER HUBERT
权利人:AMYLIN PHARMACEUTICALS INC
摘要:The present invention provides methods of assembling oligopeptides or polypeptides in a native chemical ligation reaction that eliminates the formation of unwanted side products resulting from the presence of an unprotected acidic C-terminal oligopeptide thioester. An important aspect of the present invention is providing side chain protected acidic C-terminal oligopeptide thioesters. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where aspartyl or glutamyl peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
专利号:US-2007082923-A1
优先权日:2005-10-05
标题:Process for the synthesis of compounds for selectin inhibition
发明人:WANG YOUCHU
权利人:WANG YOUCHU
摘要:The present teachings relate to the field of anti-inflammatory substances, and more particularly to the preparation of compounds that act as antagonists of the mammalian adhesion proteins known as selecting. In some embodiments, the present teachings provide methods for preparing compounds for treating selectin-mediated disorders that have the formula VI: n n nwherein R 1 , R 2 , R 3 , p, and q are defined herein.
专利号:WO-9526975-A1
优先权日:1994-03-30
标题 :Acyclic aliphatic branched alkyl groups as constituents of protective groups bound to side chains of amino-acid moieties, and their use in the preparation of peptide, polypeptide or protein structures
发明人:UNDEN ANDERS
权利人:UNDEN ANDERS
摘要:A protective group bound to a side chain of an amino-acid moiety, which group is an aliphatic acyclic branched alkyl group protecting a thiol, hydroxyl, or carboxyl group or an aliphatic acyclic branched alkoxycarbonyl group protecting an amino group or heterocyclic nitrogen, wherein the alkyl and alkoxy entities have from 6 to 18 carbon atoms and have at least two identical alkyl chains, is described. Further, the use of such a protective group bound to a side chain of an amino-acid moiety in the synthesis of peptides, polypeptides and proteins is disclosed.
专利号:US-7635749-B2
优先权日:1999-12-24
标题 :Methods and compositions for prolonging elimination half-times of bioactive compounds
发明人:DENNIS MARK S; LOWMAN HENRY B; DELANO WARREN L
权利人:GENENTECH INC
摘要:Peptide ligands having affinity for IgG or for serum albumin are disclosed. Also disclosed are hybrid molecules comprising a peptide ligand domain and an active domain. The active domain may comprise any molecule having utility as a therapeutic or diagnostic agent The hybrid molecules of the invention may be prepared using any of a number techniques including production in and purification from recombinant organisms transformed or transfected with an isolated nucleic acid encoding the hybrid molecule, or by chemical synthesis of the hybrid. The hybrid molecules have utility as agents to alter the elimination half-times of active domain molecules. Elimination half-time is altered by generating a hybrid molecule of the present invention wherein the peptide ligand has binding affinity for a plasma protein. In a preferred embodiment, a bioactive molecule having a short elimination half-time is incorporated as or into an active domain of the hybrid molecules of the invention, and the binding affinity of the peptide ligand domain prolongs the elimination half-time of the hybrid as compared to that of the bioactive molecule.