对硝基苯乙腈置于硫酸,铁粉,氯化铵,溶剂黄146体系中,化学反应生成对氨基苯乙酸 参考文献:Design,Synthesis And Biological Evaluation Of Novel Sesquiterpene Mustards As Potential Anticancer Agents 标题:Design,Synthesis And Biological Evaluation Of Novel Sesquiterpene Mustards As Potential Anticancer Agents 摘要:Several Novel Series Of Sesquiterpene Mustards (Sms) Bearing Nitrogen Mustard And Glutathione (Gsh)-Reactive Alpha-Methylene-Gamma-Butyrolactone Groups Were Successfully Prepared For The First Time And Showed Excellent Antiproliferative Activities In Vitro. Among Them,Compounds 2E And 2G Displayed The Highest Antiproliferative Properties With Ic50 Values Ranging From 2.5 To 8.7 Mu M. The Selectivity Of These Two Compounds Was Evaluated By Srb Method Against Human Cancer And Normal Hepatic Cells (Hepg2 And L02). The Induction Of Apoptosis And Effects On The Cell Cycle Distribution With Compounds 2E And 2G Were Investigated By Hoechst 33,258 Staining And Flow Cytometry,Which Exhibited That They Could Induce Selective Cell Apoptosis And Cell Cycle Arrest In Hepg2 And L02 Cells. In Addition,Further Investigation Showed That Compounds 2E And 2G Could Obviously Inhibit The Proliferation Of Hepg2 Cells By Inducing Significant Dna Cross-Linking And Depleting Gsh In Cell Media. The Good Cytotoxicity And Selectivity Of Compounds 2E And 2G Pointed Them As Promising Leads For Anticancer Drug Design. (C) 2015 Published By Elsevier Masson Sas. Doi:10.1016/j.Ejmech.2015.03.001
专利号:US-2012165520-A1 优先权日:2010-12-23 标题:Process for the synthesis of prodrugs of opioids 发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
专利号:EP-0310950-B1 优先权日:1983-11-18 标题 :Quinoline intermediates for the synthesis of 1H-imidazo[4,5-c]quinolines and 1H-imidazo[4,5-c]quinolin-4-amimes 摘要:Compounds of the types (I) and (II) are disclosed, wherein each R5 is independently selected from the group consisting of alkyl of one to about four carbon atoms, alkoxy of one to about four carbon atoms and halogen, and n is an integer from 0 to 2, with the proviso that if n is 2, then said R5 substituents together contain no more than 6 carbon atoms; R6 is selected from the group consisting of hydroxyalkyl of one to about six carbon atoms and cyclohexylmethyl; and R7 is selected from the group consisting of alkyl of one to about four carbon atoms and hydrogen. These compounds may be used as intermediates for the synthesis of 1H-imidazo[4,5-c]quinoline derivatives.
专利号:US-9206222-B2 优先权日:2009-06-29 标题:Solid phase peptide synthesis of peptide alcohols 发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN 权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
专利号:US-3732199-A 优先权日:1971-03-15 标 题 :Peptide synthesis 发明人:SCHWARZ J 权利人:SQUIBB & SONS INC 摘要:IMPROVEMENT IN THE SYNTHESIS OF PEPTIDES INVOLVING THE FORMATION OF NOVEL ACTIVE INTERMEDIATES. THESE ACTIVE INTERMEDIATES ARE FORMED BY REACTION AT LOWERED TEMPERATRES OF AN IMIDYL HALIDE WITH THE TERTIARY AMMONIUM SALT OF THE ACID MOIETY OF AN AMINO ACID OR PEPTIDE. THE INTERMEDIATE THUS FORMED IS THEN REACTED WITH THE AMINO MOIETY OF THE AMINO ACID OR PEPTIDE TO BE COUPLED, THUS FORMING THE DESIRED PEPTIDE OR POLYPEPTIDE.
专利号:US-5527824-A 优先权日:1985-07-22 标题 :Substituted Di-T-Butlyphenols useful for inhibiting leukotriene synthesis 发明人:SCHERRER ROBERT A 权利人:RIKER LABORATORIES INC 摘要:Substituted Di-T-Butylphenols useful for inhibiting the synthesis of leukotrienes are disclosed.
专利号:US-9890126-B2 优先权日:2012-04-24 标 题:Synthesis of novel inhibitors of isoprenoid biosynthesis (ISPF) 发明人:HAGEN TIMOTHY J; ZHANG ZHENG; LAZOWSKI ZACHARY; CLARE MICHAEL; BEGLEY DARREN W 权利人:UNIV NORTHERN ILLINOIS BOARD OF TRUSTEES; BERYLLIUM DISCOVERY CORP 摘要:Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.
[参考文献]: Ahmed H Bedair, Et Al. Preparation Of 4-Aminophenylacetic Acid Derivatives With Promising Antimicrobial Activity. Acta Pharm. 2006 Sep;56(3):273-84. [参考文献]: C S Temple, Et Al. Peptide Mimics As Substrates For The Intestinal Peptide Transporter. J Biol Chem. 1998 Jan 2;273(1):20-2. [参考文献]: D Meredith, Et Al. 4-Aminomethylbenzoic Acid Is A Non-Translocated Competitive Inhibitor Of The Epithelial Peptide Transporter Pept1. J Physiol. 1998 Nov 1;512 ( Pt 3)(Pt 3):629-34. [参考文献]: Hongye Zhang, Et Al. P-Aminophenylacetic Acid-Mediated Synthesis Of Monodispersed Titanium Oxide Hybrid Microspheres In Ethanol Solution. J Colloid Interface Sci. 2009 Oct 15;338(2):468-73.
合成参考文献
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