在 苄胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 1.5H,以15%的收率获得产物二甘醇胺 参考文献:Synthesis Of Fluorous Photolabile Aldehyde And Carbamate And Alkyl Carbamate Protecting Groups For Carbohydrate-Associated Amines 标题:Synthesis Of Fluorous Photolabile Aldehyde And Carbamate And Alkyl Carbamate Protecting Groups For Carbohydrate-Associated Amines 摘要:Two New Fluorous Photolabile-Protecting Groups (Fnbc And Fnb) And A New Base-Labile Protecting Group (Foc) For The Masking Of Amines Are Reported. The Protecting Groups Survive A Wide Range Of Common Reaction Conditions Used In Oligosaccharide Synthesis And Render The Attached Molecules Amenable To Fluorous Solid-Phase Extraction (Fspe). A Glycosyl Acceptor Containing The Fnb Group Is Shown To Be Useful In The Synthesis Of Carbohydrates Tagged With Free Deactivated Secondary Amines. DOI:10.1021/ol500023Y
专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-8415510-B2 优先权日:2008-02-28 标题 :Synthesis of a PEG-6 moiety from commercial low-cost chemicals 发明人:ENGELL TORGRIM 权利人:ENGELL TORGRIM; GE HEALTHCARE LTD 摘要:The present invention provides novel synthesis's for obtaining a protecting group aminoxy PEG-6 linker from cost effective, and readily available starting materials and chemicals or modified polyethylene glycols. More specifically, a novel synthesis of obtaining a modified Boc-protected aminoxy PEG-6 linker was achieved so that said linker may be attached to a vector such as a peptide based fragment.
专利号:US-8536375-B2 优先权日:2008-12-22 标题:Synthesis of obtaining modified polyethylene glycol intermediates 发明人:ENGELL TORGRIM 权利人:ENGELL TORGRIM; GE HEALTHCARE LTD 摘要:The present invention provides novel and more efficient synthesis's for obtaining an intermediate in the synthesis of obtaining a protecting group aminoxy PEG linker.
专利号:WO-0140193-A1 优先权日:1999-12-03 标题:Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.
专利号:US-2002103381-A1 优先权日:2000-11-30 标 题 :Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.
专利号:US-5919971-A 优先权日:1996-11-22 标题:Process for the synthesis of 3-mercaptopropionic acid esters 发明人:ARRETZ EMMANUEL 权利人:ELF AQUITAINE EXPLORATION PROD 摘要:This process for the synthesis of 3-mercaptopropionic acid esters by addition reaction of H2S to the corresponding acrylic acid ester is carried out in the presence of a solid-support functionalized with basic guanidine functional groups, on condition that these groups are free of hydrogen that is directly attached to a nitrogen atom.
1: Pignatello R, Impallomeni G, Pistarà V, Cupri S, Graziano AC, Cardile V, Ballistreri A. New amphiphilic derivatives of poly(ethylene glycol) (PEG) as surface modifiers of colloidal drug carriers. III. Lipoamino acid conjugates with carboxy- and amino-PEG(5000) polymers. Mater Sci Eng C Mater Biol Appl. 2015 Jan;46:470-81. doi: 10.1016/j.msec.2014.10.054. Epub 2014 Oct 23. doi: 10.1039/c0cc02615h. Epub 2010 Nov 26. doi: 10.1016/j.jpba.2010.07.008. Epub 2010 Aug 1. doi: 10.1039/b811818c. Epub 2008 Sep 16.
合成参考文献
摘要:Gigiena Truda i Professional'nye Zabolevaniya. Labor Hygiene and Occupational Diseases., 32(9)(50), 1988 摘要:U.S. Department of Health and Human Services, Public Health Service, Center for Disease Control, National Institute for Occupational Safety Health. Registry of Toxic Effects of Chemical Substances (RTECS). National Library of Medicine's current MEDLARS file., p. 85/8407 摘要:IMDG; International Maritime Dangerous Goods Code; International Maritime Organization p.8109 (1988)