2-氯苯甲酸甲酯置于盐酸,乙醚,Calcium Chloride,苯体系中,化学反应生成 氯代(邻氯苯基)二苯基甲烷 参考文献:Gomberg; Van Slyke,Journal Of The American Chemical Society,1911,Vol. 33,P. 533 标题:Gomberg; Van Slyke,Journal Of The American Chemical Society,1911,Vol. 33,P. 533
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-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-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:WO-2024182268-A1 优先权日:2023-02-27 标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics 发明人:HAN AMY 权利人:REGENERON PHARMA 摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.
专利号:US-2002019013-A1 优先权日:1999-03-08 标 题:Combined resin method for high-speed synthesis of combinatorial libraries 发明人:LOU BOLIANG; GHARBAOUI TAWFIK 摘要:A method for high-speed parallel synthesis of combinatorial libraries is disclosed where two or more resins of dissimilar functionality are combined in the same reaction vessel in which a plurality of chemical reactions are carried out to create multiple compounds which are then sequentially and individually cleaved from the different resins under the appropriate cleavage conditions for each resin. As used herein resins are considered different when they exhibit different chemical activity in the presence of cleaving or releasing agents. The resins are different when the individual resins have either dissimilar polymeric backbones or dissimilar linkers or both and thus have a different chemical activity in the presence of a release or cleaving agent from the other resins in the reaction vessel.
专利号:US-2020247841-A1 优先权日:2017-09-27 标 题 :Synthesis of icatibant 发明人:RAMU VASANTHAKUMAR GANGA; PATIL NITIN SOPANRAO; PALLE VENTAKA RAGHAVENDRACHARYUL; Yogesha 权利人:BIOCON LTD 摘要:The present invention relates to the efficient solid-phase synthesis of Icatibant represented by Formula (I). The present invention relates to an efficient process for the preparation of Icatibant by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare Icatibant. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to ensure complete removal of piperidine and reactions are going for completion, and thus avoid addition/deletion sequences and also improve the process yield.
参考文献:10.1002/cmdc.201100144 摘要:Su X, Vicker N, Thomas MP, Pradaux-Caggiano F, Halem H, Culler MD, Potter BV. Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors. ChemMedChem. 2011 Aug 01;6(8):1439–51.