CAS: 23138-64-9; 3-Acetylphenylisocyanate

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CAS号99-03-6 3'-氨基苯乙酮 | CAS号503-38-8 氯甲酸三氯甲酯 | CAS号86764-52-5 3-(3-acetylphen... | CAS号86781-34-2 3-(3-acetylphen...

三光气,间氨基苯乙酮 以 四氢呋喃 用作溶剂,化学反应 3.5H,反应生成异氰酸3-乙酰基苯酯
参考文献:含5-氟吲哚-2-酮部分的苯脲的设计,合成及抗肿瘤评估
标题:含5-氟吲哚-2-酮部分的苯脲的设计,合成及抗肿瘤评估
摘要:背景:新型抗肿瘤药的开发仍然非常需要. 目的:本研究的重点是带有5-氟吲哚-2-酮部分的苯基脲的设计,合成和抗肿瘤评估. 方法:设计并合成了三套苯基脲,并通过mtt法测定了它们对四种人类癌细胞系(hela,Eca-109,A549和mcf-7)的抗增殖能力.在人乳腺癌的异种移植模型(mcf-7)中进一步评估了体内抗癌活性. 结果:总共合成了二十一种新化合物,并通过1H和13C NMR以及hr-Ms进行了表征.最初构建了三组化合物(1A‒1C,2A‒2C和3A‒3C),并评估了这些分子对hela,Eca-109,A549和mcf-7的初步抗增殖活性,突出了间位取代的苯基脲(1A‒1C)是最具细胞毒性的药物.然后设计并合成了一系列间位取代的苯基脲衍生物(1D‒1O)用于结构-活性关系研究.大多数新化合物显示出理想的细胞毒性,其中化合物1G对测试的人类癌细胞表现出最显着的细胞毒性作用,Ic50值为1
Doi:10.2174/1573406416666200206123319

专利信息

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-9700244-A1
优先权日:1995-06-19
标题 :Process for parallel synthesis of a non-peptide library
发明人：FRITZ JAMES E; KALDOR STEPHEN W
权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W
摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.

专利号:US-2005192265-A1
优先权日:2003-03-20
标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:US-6906056-B2
优先权日:1998-06-22
标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J
权利人:LILLY CO ELI
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:US-2022010060-A1
优先权日:2018-12-12
标题:Polycarbonate polyols
发明人：FENG XIAOSHUANG; PATIL NAGANATH; BOOPATHI Senthil; GNANOU YVES; HADJICHRISTIDIS NIKOS
权利人:UNIV KING ABDULLAH SCI & TECH
摘要:Embodiments of the present disclosure describe polymerization systems for the synthesis of polycarbonate polyols, methods of synthesizing polycarbonate polyols using the polymerization systems, methods of recovering initiators and/or activators for use or re-use in the synthesis of polycarbonate polyol, and the like. The polymerization systems can comprise an initiator including a mono- or multi-functional carboxylate or carbonate salt having an organic cation as a counter-ion; an optional co-initiator including a mono- or multi-functional protic compound selected from acids, alcohols, water, and combinations thereof; and an activator including a borane compound selected from alkyl boranes and aryl boranes; wherein the activator and one or more of the initiator and co-initiator associate to form an ate complex.

专利号:EP-0789577-A1
优先权日:1995-06-07
标 题:Synthesis of n-substituted oligomers