N-苄基乙酰胺置于盐酸,Sodium Hydroxide,Tin,硫酸,硝酸体系中,化学反应 2.83H,反应生成 4-氨基苄胺 参考文献:Ph Optimization Of Nucleophilic Reactions In Water 标题:Ph Optimization Of Nucleophilic Reactions In Water 摘要:We Present A Way Of Prescribing The Ph For A Reaction So As To Obtain Either (A) Maximum Yield In Competition With Hydrolysis Or (B) Selective Reaction At Either Of Two Sites In Such Nucleophile-Electrophile Reactions As C-Alkylation Of Acidic Ketones And The Acylation And Sulfonylation Of Amines. First,We Derive The Following General Equation For Ph(Max),The Ph Giving The Highest Yield Of The Product (P) Of The Reaction Of A Nucleophile (Nu) With A Hydrolyzable Electrophile (E) In Water: Ph(Max) = 1/2[log (K(W)/k(Oh)) + Pk(W) + Pk(A)] (K(W) And K(Oh) Refer To The Water-And Hydroxide-Promoted Hydrolyses Of E,K(W) Is The Autoprotolysis Constant Of Water,And K(A) Is The Acid Dissociation Constant Of Nuh+,The Conjugate Acid Of Nu). Ph(Max) Thus Depends On A Property Of E (Namely,K(W)/k(Oh)) And A Property Of Nu (The Pk(A) Of Nuh+),But Not On The Rate Constant For The Reaction Of E With Nu Or The Concentration Of Nu. We Then Deduce Analogous Approximate Equations For Maximum Selectivity For Reaction At Either Of Two Nucleophilic Sites,Specifically,Equations Giving Ph(Xmax) And Ph(Ymax),The Ph Values For The Maximum Yields Of The Respective Products (P(X) And P(Y)) Of The Reactions Of E With The Two Nucleophiles. We Find That (A) Ph-Yield Profiles Calculated From The Equations Concur With Observed Yields For Reactions Under Pseudo-First-Order Conditions And (B) Preparative Experiments At The Estimated Ph Values Give Good To Excellent Yields Of Clean Products And High Selectivity In Both The C-Alkylation And Schotten-Baumann Reactions. DOI:10.1021/ja00034A040
专利号:WO-0140193-A1 优先权日:1999-12-03 标题:Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.
专利号:US-2002103381-A1 优先权日:2000-11-30 标 题 :Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-4895954-A 优先权日:1986-07-26 标题 :Precursors for synthesis of triphendioxazine dyestuffs 发明人:SCHWAIGER GUENTHER; SPRINGER HARTMUT; HELMLING WALTER 权利人:HOECHST AG 摘要:Water-soluble triphendioxazine compounds which have fiber-reactive properties as dyestuffs, which afford deep and fast dyeings on fiber materials, such as wool and, in particular, cellulose, and which correspond to the formula (1) ##STR1## in which: n is the number 0 or 1; n Y is the vinyl group or an ethyl group containing, in β-position, a substituent which can be eliminated by means of an alkali; n Q 1 and Q 2 both represent a benzotriazole radical which can also be additionally substituted in the benzene nucleus by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halogen, carboxy or sulfo; n B is --O--, --S--, --NH-- or --N(R')-- wherein R' is optionally substituted alkyl having 1 to 6 carbon atoms; n W 1 and W 2 both represent a divalent, optionally substituted aliphatic, cycloaliphatic, aliphatic-cycloaliphatic, araliphatic or aromatic-carbocyclic radical, it being possible for the aliphatic radicals to be interrupted by hetero groups --O--, --S--, --SO 2 --, --CO--, 1,4-piperidino, --NH-- and/or --N(R o )-- in which R o is optionally substituted alkyl having 1 to 6 carbon atoms or alkanoyl having 2 to 5 carbon atoms, and/or for aliphatic and aryl radicals to be attached to one another through such a hetero group; n R is hydrogen, alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms, halogen, carboxyl or sulfo; n E is hydrogen, sulfo, carboxyl, a group --SO 2 --Y as defined above or an optionally substituted sulfonamide group; and n X 1 and X 2 are both hydrogen or halogen, cycloalkyl, alkoxy, aryloxy, aryl or another substituent; n and at least one carboxy, sulfo or sulfato group is present in the molecule (1), n and pre-products of those triphendioxazine compounds, of the general formula ##STR2## in which K is an amino or nitro group, Y' is β-hydroxyethyl or defined as for Y, W has one of the meanings of W 1 , and E' is hydrogen, sulfo, carboxy or a group of the formula --SO 2 --Y' defined above, or an optionally substituted sulfonamide group, and R, B and R* have the above meanings.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:US-2013102730-A1 优先权日:2010-04-02 标 题:Polyamine-containing polymers and methods of synthesis and use 发明人:JOST ROBERT W; ULUDAG HASAN; BOLUK MEHMET YAMAN 权利人:JOST ROBERT W; ULUDAG HASAN; BOLUK MEHMET YAMAN; ALBERTA INNOVATES TECHNOLOGY FUTURES 摘要:The present invention relates to polyamine-containing polymers and methods of their synthesis and use. The polymer may be hydroxyethylcellulose, dextran, poly(vinyl alcohol) or poly(methyl acrylate).
[参考文献]: Nedjla Zehani, Et Al. Highly Sensitive Electrochemical Biosensor For Bisphenol A Detection Based On A Diazonium-Functionalized Boron-Doped Diamond Electrode Modified With A Multi-Walled Carbon Nanotube-Tyrosinase Hybrid Film. Biosens Bioelectron. 2015 Dec 15:74:830-5. [参考文献]: Steven Earl Kooi, Et Al. Electrochemical Modification Of Single Carbon Nanotubes. Angew Chem Int Ed Engl. 2002 Apr 15;41(8):1353-5. [参考文献]: Tony Breton, Et Al. Modification Of Carbon Electrode With Aryl Groups Having An Aliphatic Amine By Electrochemical Reduction Of In Situ Generated Diazonium Cations. Langmuir. 2008 Aug 19;24(16):8711-8.
合成参考文献
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