专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
专利号:US-7423154-B2 优先权日:2001-03-07 标 题 :Asymmetric process for the preparation of diarylethylpiperazines derivatives and novel asymmetric diarylmethylamines as intermediates 发明人:BROWN WILLIAM; PLOBECK NIKLAS 权利人:ASTRAZENECA AB 摘要:An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.
专利号:US-2009099061-A1 优先权日:2006-01-27 标 题:Synthesis of carotenoid analogs or derivatives with improved antioxidant characteristics 发明人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 权利人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 摘要:A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
专利号:US-5670465-A 优先权日:1993-01-08 标题 :Preparation of p-fuchsones and synthesis of p-dihydroxylated aromatic compounds therefrom 发明人:COSTANTINI MICHEL; MANAUT DANIEL; MICHELET DANIEL 权利人:RHONE POULENC CHIMIE 摘要:p-Dihydroxylated aromatic compounds are prepared via the oxidation of p-fuchsones, the latter advantageously being synthesized by reacting a phenolic compound having at least one hydrogen atom in the para-position to the hydroxyl function with a non-enolizable ketonic compound, in the presence of a catalytically effective amount of an acid catalyst and, optionally, a cocatalytically effective amount of an ionizable sulfur-containing compound.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2023117370-A1 优先权日:2020-04-17 标 题:Regioselective synthesis of substituted compounds 发明人:BEAUDRY CHRISTOPHER M; ZHANG XIAOJIE 权利人:UNIV OREGON STATE 摘要:Disclosed herein are embodiments of a method for making substituted compounds with specific and selectable regiochemistry. Also disclosed are compounds made by the method. The method may comprise contacting a compound having a formula Iwith a compound according to formula IIin the presence of a Lewis acid to form a phenol compound according to formula III and/or a benzofuranone compound according to formula IV
[参考文献]: Alfonso Pérez-Garrido, Et Al. Convenient Qsar Model For Predicting The Complexation Of Structurally Diverse Compounds With Beta-Cyclodextrins. Bioorg Med Chem. 2009 Jan 15;17(2):896-904. [参考文献]: Cynthia D Selassie, Et Al. Cellular Apoptosis And Cytotoxicity Of Phenolic Compounds: A Quantitative Structure-Activity Relationship Study. J Med Chem. 2005 Nov 17;48(23):7234-42. [参考文献]: E J Routledge, Et Al. Structural Features Of Alkylphenolic Chemicals Associated With Estrogenic Activity. J Biol Chem. 1997 Feb 7;272(6):3280-8.
合成参考文献
摘要:Beier, P., Science of Synthesis Knowledge Updates, (2014) 2, 287. 摘要:Bartels, F.; Zimmer, R.; Christmann, M., Science of Synthesis Knowledge Updates, (2017) 3, 238. 摘要:González-Bello, C., Science of Synthesis Knowledge Updates, (2018) 1, 211. 摘要:Allen, C. C. R., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 9. 摘要:Ros, A.; Fernández, R.; Lassaletta, J. M., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 436.