📜2-甲基咪唑啉 以 水 用作溶剂,化学反应 0.17H,反应生成N-乙酰基乙二胺 参考文献:Chinon-Amin-Reaktionen,4. 手套.2,3,4-Trihydro-Benzo[f]Chinoxalin-6-One 标题:Chinon-Amin-Reaktionen,4. 手套.2,3,4-Trihydro-Benzo[f]Chinoxalin-6-One 摘要:1,4-Naphthochinone 2 Reagieren Mit Ethylendiamin (3) Zu 5-Substituierten 2,3,4-Trihydro-Benzo[f]-Chinoxalin-6-Onen 7. Die类似物 Reaktionen Mit N-Acetyl-Ethylendiamin (12) Zeigen,Daß Die Amino-1,4-Naphthochinone 6 Und Nicht Die 1,4-Naphthochinon-Imine 4 Zwischenstufen Sind.Die Verbindungen 6 Entstehen Nach Einem Additions-Enolisierungs-Oxidations-Oder Additions-Eliminierungs-Mechanismus.Beide Mechanismen Doi:10.1002/ardp.19803130705
专利信息
专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
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: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-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:WO-0078725-A1 优先权日:1999-06-18 标题 :Synthesis of substituted amidines 发明人:CHOUEIRY DANIELE; GIRAUD DANIEL LIONEL; SCHOTTEN THEO 权利人:LILLY CO ELI; CHOUEIRY DANIELE; GIRAUD DANIEL LIONEL; SCHOTTEN THEO 摘要:The present invention provides a process for preparing amidines starting from carboxylic acid derivatives, in which the carboxylic acid containing moiety is attached to a sp3-, or sp 2- or sp1¿-hybridized carbon atom. The sp2-hybridized carbon atom, to which the carboxylic acid containing moiety is attached to may be part of an aromatic or heteroaromatic or olefinic system.
[参考文献]: Emma J Wright, Et Al. Design Of Maleimide-Functionalised Electrodes For Covalent Attachment Of Proteins Through Free Surface Cysteine Groups. Chemistry. 2014 May 5;20(19):5550-4.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 312. 摘要:Dekeukeleire, S.; D'hooghe, M.; De Kimpe, N., Science of Synthesis Knowledge Updates, (2011) 3, 151. 摘要:R. B. Martin and A. Parcell. J. Am. Chem. Soc. 83, 4830 (1961). 摘要:H. K. Hall. J. Phys. Chem. 60, 63 (1956). 摘要:Yamashita, M., Science of Synthesis: Knowledge Updates, (2023) 2, 42.