CAS: 109-90-0; Ethyl Isocyanate

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丙酸置于叠氮磷酸二苯酯,三乙胺体系中,用 甲苯 用作溶剂,化学反应 1.25H,反应生成异氰酸乙酯
参考文献:Structure-Based Drug Design And Potent Anti-Cancer Activity Of Tricyclic 5:7:5-Fused Diimidazo[4,5-D:4',5'-F][1,3]Diazepines
标题:Structure-Based Drug Design And Potent Anti-Cancer Activity Of Tricyclic 5:7:5-Fused Diimidazo[4,5-D:4',5'-F][1,3]Diazepines
摘要:Judicial Structural Modifications Of 5: 7-Fused Ring-Expanded Nucleosides (Rens),Based On Molecular Modeling Studies With One Of Its Known Targets,Human Rna Helicase (Hddx3),Led To The Lead,Novel,5:7-5-Fused Tricyclic Heterocycle (1). The Latter Exhibited Promising Broad-Spectrum In Vitro Anti-Cancer Activity Against A Number Of Cancer Cell Lines Screened. This Paper Describes Our Systematic,Albeit Limited,Structure-Activity Relationship (Sar) Studies On This Lead Compound,Which Produced A Number Of Analogs With Broad-Spectrum In Vitro Anti-Cancer Activities Against Lung,Breast,Prostate,And Ovarian Cancer Cell Lines,In Particular Compounds 15I,15J,15M And 15N Which Showed Ic50 Values In Submicromolar To Micromolar Range,And Are Worthy Of Further Explorations. The Sar Data Also Enabled Us To Propose A Tentative Sar Model For Future Sar Efforts For Ultimate Realization Of Optimally Active And Minimally Toxic Anti-Cancer Compounds Based On The Diimidazo[4,5-D:4',5'-F][1,3]Diazepine Structural Skeleton Of The Lead Compound 1. (C) 2012 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2012.11.050

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-6924385-B2
优先权日:2002-11-18
标 题:Method for synthesis of aliphatic isocyanates from aromatic isocyanates
发明人：LETTMANN CHRISTIAN; KOHLSTRUK STEPHAN; STOCHNIOL GUIDO; SPYROU EMMANOUIL
权利人:DEGUSSA
摘要:The invention relates to a method for synthesis of aliphatic isocyanates from aromatic isocyanates in substantially 3 stages. In particular, the invention relates to a method for synthesis of bis{4-isocyanatocyclohexyl}methane (H 12 MDI) from bis{4-isocyanatophenyl}methane (MDI). More especially, the invention relates to a method for synthesis of H 12 MDI with a trans-trans isomer content of <30%, preferably of <20%, particularly preferably of 5 to 15%.

专利号:US-7825244-B2
优先权日:2005-06-10
标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
发明人：BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG
权利人:JANSSEN PHARMACEUTICA NV
摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.

专利号:US-12338202-B2
优先权日:2021-09-10
标 题 :One pot synthesis of urea (meth)acrylates
发明人：BESTGEN SEBASTIAN; BEYER SILVIA
权利人:EVONIK OPERATIONS GMBH
摘要:A one-pot synthesis of polymerizable and acyclic urea (meth)acrylates, preferably mono(meth)acrylates, can be performed via in-situ synthesis of urea alcohols or amines followed by direct reaction with a (meth)acrylate reactive diluent. The urea alcohol/amine is obtained from isocyanates and alcohols, amines, or hydroxyamines. Subsequently, the reaction with the (meth)acrylate reactive diluent takes place and the urea (meth)acrylate is directly obtained either in solution with the reactive diluent, or as a pure material after removal of the reactive diluent.

专利号:US-4472568-A
优先权日:1981-11-12
标 题:Process for the preparation of polyamines from N-monoaryl-N',N'-dialkyl urea compounds and their use for the synthesis of polyurethanes
发明人：RASSHOFER WERNER; GROEGLER GERHARD
权利人:BAYER AG
摘要:This invention relates to an improved process for the preparation of aromatic polyamines containing urethane and/or biuret and/or urea and/or isocyanurate groups and preferably also ether groups by the hydrolysis of poly-N-monoaryl-N',N'-dialkyl urea compounds (1-aryl-3,3-dialkyl ureas). The ureas are obtained by the reaction of secondary aliphatic, cycloaliphatic or saturated heterocyclic amines with divalent to tetravalent isocyanate compounds containing isocyanate end groups attached to aromatic residues. The ureas correspond to the general formula: wherein R1, R2 denote alkyl or cycloalkyl groups, or together form a ring and A denotes a divalent to tetravalent residue attached to the ureas by aromatic groups. Hydrolysis is carried out in the presence of water and up to two equivalents of a base containing hydroxide ions and/or up to two equivalents of a compound containing tertiary amino groups, optionally in the presence of solvents. The use of the polyamines obtained by this process for the synthesis of polyurethanes is also described.

专利号:US-5714127-A
优先权日:1992-10-08
标题 :System for multiple simultaneous synthesis
发明人：DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J
权利人:WARNER LAMBERT CO
摘要:A system for the multiple, simultaneous synthesis of compounds preferably uses a reaction apparatus comprising a reservoir rack having a plurality of reaction wells, a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends, a holder block, having a plurality of apertures, and a manifold, which has ports to allow introduction/maintenance of a controlled environment. The manifold top wall has a plurality of apertures in axial alignment with the reaction tubes and a gasket which allows penetration by a needle in order to dispense and aspirate materials from the reaction tubes. Sealing members, such as gaskets, are placed between the holder block, manifold and reservoir rack and the components are releasably fastened together. A robotic sample processor is used to automate the synthesis process using the reaction apparatus.