📜丙二酸,3,4-二氯苯甲醛置于哌啶,吡啶体系中,化学反应 6.0H,反应生成3,4-二氯肉桂酸 参考文献:Synthesis And Sar Study Of Diarylpentanoid Analogues As New Anti-Inflammatory Agents 标题:Synthesis And Sar Study Of Diarylpentanoid Analogues As New Anti-Inflammatory Agents 摘要:合成了97系列二苯基戊烷类化合物,并通过使用γ干扰素(ifn-γ)/脂多糖(lps)刺激的raw264.7巨噬细胞进行no抑制试验评估其抗炎活性.12个化合物(9,25,28,43,63,64,81,83,84,86,88和97)与姜黄素(14.7 +/-0.2 µm)相比显示出更大或相似的no抑制活性,特别是化合物88和97,它们表现出最显著的no抑制活性,Ic50值分别为4.9 +/-0.3 µm和9.6 +/-0.5 µm.结构-活性关系(sar)研究表明,两个芳香环上羟基的存在对这些分子的生物活性至关重要.除了多酚类衍生物外,A环上低电子密度和b环上高电子密度对提高no抑制作用很重要.同时,药效团映射表明,B环上间位和对位上的羟基取代可能是高活性二苯基戊烷类化合物的标记. Doi:10.3390/molecules191016058
专利号:US-6268535-B1 优先权日:1998-01-09 标题 :Synthesis of 3-aryl-1-indanamines 发明人:MOUSSA ADEL M; HAIDER REEM; TAFT HEATHER; JURAYJ JURJUS; WANG WEIHENG; SUH HAESUK 权利人:PHARM ECO LAB INC 摘要:The present invention is a method of preparing a 3-aryl-1-indanamine represented by structural formula I:and physiologically acceptable salts thereof.In structure I, phenyl ring A can be unsubstituted or substituted with 1-4 substitutents.R1 is an aromatic group which can be substituted or unsubstituted.R2 and R3 are each, independently, hydrogen, an aliphantic group, a substituted aliphatic group, an aromatic group, a substituted aromatic group, an aralkyl group, or a substituted aralkyl group. Alternatively, R2 and R3, taken together with the nitrogen substitutent on the indan ring, form a non-aromatic ring system having 1-2 heteroatoms.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-5089639-A 优先权日:1988-09-01 标题:N-cycloalkylalkylamines, process for their preparation, their use as a medicament and their synthesis intermediates 发明人:AUBARD GILBERT G; CALVET ALAIN P; DEFAUX JEAN-PIERRE; GOURET CLAUDE J; GROUHEL AGNES M; JACOBELLI HENRY L; JUNIEN JEAN-LOUIS; PASCAUD XAVIER B; ROMAN FRANCOIS F; HUDSPETH JAMES P; LIN YUAN 权利人:JOUVEINAL SA 摘要:N-Cycloalkylalkylamines of formula I: ##STR1## in which: R1 is phenyl which is optionally mono-, di- or trisubstituted by halogens or lower alkyl, haloalkyl or lower alkoxy radicals, or is an aromatic heterocyclic radical having 5 to 7 chain members, in which the hetero atom is nitrogen, oxygen or sulphur, n R2 is lower alkyl, n R3 is hydrogen or lower alkyl, n m has the value of 1 or 2, n R4 is cycloalkyl --CH(CH2)n, in which a carbon atom may carry a radical Rx, which is lower alkyl or phenyl; and in which n has the values from 2 to 5, n R5 is phenyl, which can be mono-, di- or trisubstituted by halogens or by lower alkoxy radicals, and n Q represents an ethylene-1,2-diyl group --CHâ•?CH-- or a cyclopropane-1,2-diyl group ##STR2##
专利号:WO-9935119-A1 优先权日:1998-01-09 标 题:Synthesis of 3-aryl-1-indanamines
专利号:US-7002020-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
[参考文献]: J Witherington, Et Al. Conformationally Restricted Indolopiperidine Derivatives As Potent Ccr2B Receptor Antagonists. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2177-80.
合成参考文献
摘要:Indian Journal of Pharmaceutical Sciences., 49(77), 1987