- Combining Flavin Photocatalysis and Organocatalysis: Metal-Free Aerobic Oxidation of Unactivated Benzylic Substrates
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We report a system with ethylene-bridged flavinium salt 2b which catalyzes the aerobic oxidation of toluenes and benzyl alcohols with high oxidation potential (Eox > +2.5 V vs SCE) to give the corresponding benzoic acids under visible light irradiation. This is caused by the high oxidizing power of excited 2b (E(2b?) = +2.67 V vs SCE) involved in photooxidation and by the accompanying dark organocatalytic oxygenation provided by the in situ formed flavin hydroperoxide 2b-OOH.
- Zelenka, Jan,Svobodová, Eva,Tarábek, Ján,Hoskovcová, Irena,Boguschová, Veronika,Bailly, Sarah,Sikorski, Marek,Roithová, Jana,Cibulka, Radek
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Read Online
- FUSED TRICYCLIC COMPOUNDS AS RAF KINASE INHIBITORS
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Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
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Paragraph 0209; 0329; 0330-0331
(2021/02/16)
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- Regulating Cofactor Balance In Vivo with a Synthetic Flavin Analogue
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A novel strategy to regulate cofactor balance in vivo for whole-cell biotransformation using a synthetic flavin analogue is reported. High efficiency, easy operation, and good applicability were observed for this system. Confocal laser scanning microscopy was employed to verify that the synthetic flavin analogue can directly permeate into Escherichia coli cells without modifying the cell membrane. This work provides a promising intracellular redox regulatory approach to construct more efficient cell factories.
- Tan, Zhuotao,Zhu, Chenjie,Fu, Jingwen,Zhang, Xiaowang,Li, Ming,Zhuang, Wei,Ying, Hanjie
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supporting information
p. 16464 - 16468
(2018/11/23)
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- CHEMICAL REGENERATION METHOD OF OXIDIZED COENZYME NAD (P)+
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It discloses a chemical regeneration method of oxidized coenzyme NAD(P)+ which is under an oxygen or air atmosphere condition, adding a catalytic amount of bridged flavin, and oxidizing NAD(P)H to obtain NAD(P)+. The catalyst for regeneration of cofactor is cheap and easily available small organic molecule having no noble metal; this regeneration system can regenerate NADH and NADPH; this regeneration system has a wide pH range and temperature range, being applicable to various oxidation reactions catalyzed by nicotinamide-dependent oxidoreductase.
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Paragraph 0047; 0050
(2017/07/06)
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- CONDENSED TRICYCLIC COMPOUNDS AS Raf KINASE INHIBITORS
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PROBLEM TO BE SOLVED: To provide specific tricyclic compounds that can be useful for inhibiting Raf kinase and for treating disorders mediated by Raf kinase. SOLUTION: A compound is represented by the general formula 1 in the figure. (Q is C or N; W is C or N; X is CH2 or O; Y is NR12, O or S; Z is O, S, NR13, CO, SO, SO2 or CR13R14; R1 to R6 are each independently hydrogen, halogen, haloalkyl, alkyl or the like.) SELECTED DRAWING: None COPYRIGHT: (C)2017,JPO&INPIT
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Paragraph 0206; 0207
(2017/01/05)
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- Condensed tricyclic compounds as RAF kinase inhibitors
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The invention provides certain condensed tricyclic compounds as well as salt, compositions and application methods thereof.
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Paragraph 0358; 0550; 0551; 0552; 0553; 0554
(2016/10/07)
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- FUSED TRICYCLIC COMPOUNDS AS RAF KINASE INHIBITORS
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Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
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Paragraph 0368-0370
(2015/02/25)
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- FUSED TRICYCLIC COMPOUNDS AS RAF KINASE INHIBITORS
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Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
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Page/Page column 70
(2013/07/19)
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- Chemoselective sulfide oxidation mediated by bridged flavinium organocatalysts
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The chemoselective oxidation of sulfides to sulfoxides, catalysed by bridged, tetracyclic flavinium catalysts is presented. The flavinium catalysts are easily prepared via a telescoped three-step process. A range of sulfoxides is accessed in excellent yield and chemoselectivity.
- Marsh, Barrie J.,Carbery, David R.
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scheme or table
p. 2362 - 2365
(2010/05/19)
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- SUBSTITUTED CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT OF DIABETES AND LIPID DISORDERS, THEIR PREPARATION AND USE
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The present invention is concerned with racemic or enantiomerically enriched substituted carboxylic acids and derivatives thereof represented by Formula 1 ; or pharmaceutically acceptable salts thereof. The present invention also includes pharmaceutical c
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Page/Page column 19
(2008/06/13)
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- Imidazopyridinone derivatives and their use as phosphodiesterase inhibitors
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A compound (Ia): wherein the variables are defined in the specification, its prodrug or a pharmaceutically acceptable salt thereof useful in the treatment of angina, hypertension etc.
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- Pyrrolyl quinoxalindiones their production and use as AMPA receptor antagonists
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Pyrrolylquinoxalinediones of the formula I and their tautomeric and isomeric forms, and their physiologically tolerated salts are described, where the variables have the following meaning: R1hydrogen, C1-C6-alkyl, substitu
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- N1,N10-Ethylene-bridged high-potential flavins: Synthesis, characterization, and reactivity
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N1,N10-Ethyleneisoalloxazinium chloride and its 8-Cl-, 7-CF3-, and 3-CH3-7-CF3-substituted analogs were synthesized for the purpose of exhibiting thermal reactivity with organic substrates. The new flavins were characterized spectroscopically and electrochemically, and were found to react with amines, thiols, and phenylhydrazine, the latter case exhibiting catalytic aerobic recycling. Reactions of aliphatic benzylic and cyclopropyl amines with the 7-CF3 analog were also compared to their oxidations by tris(phenanthroline)iron(III). All reactions of the flavinium salts appear to occur through heterolytic rather than homolytic mechanisms.
- Li, Wen-Shan,Zhang, Nanjing,Sayre, Lawrence M.
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p. 4507 - 4522
(2007/10/03)
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- The synthesis and some reactions OF 3-(2-aminophenyl)-2-iminothiazolidines. Ring closure of n-(2-thiocyanaoethyl,)-nphenylenediamines; thiazolidine vs. 3,1,6-benzothiadiazocine formation
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When treated with strong acids, the N-(2-thiocyanatoethyl)-n-phenylenediamines (1g-1y) are cyclized exclusively to 3-(2-aninophen- yl)-2-iminothiazolidines (6) while the related tertiary amines (1a-1f) gave, under the same conditions, benzothiadiazocines
- Hornyak,Bertha,Zauer,Lempert,Feller,Pjeczka
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p. 2009 - 2030
(2007/10/02)
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- 2-nitroaniline derivatives
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2-nitroaniline derivatives of the general formula I: STR1 in which R1 and R2 represent, independent of one another, hydrogen, an alkyl of 1 to 4 carbon atoms, a monohydroxyalkyl of 2 to 4 carbon atoms or a dihydroxyalkyl of 3 or 4 carbon atoms, provided that R1 and R2 do not simultaneously represent alkyl groups of 1 to 4 carbon atoms, and X denotes an alkyl, monohydroxyalkyl, perfluoroalkyl or halogen, for use as an agent in a hair dyeing composition. Also disclosed are new 2-nitroaniline derivatives of the general formula II: STR2 in which Ra and Rb denote, independent of one another, ethyl, a monohydroxylalkyl of 2 to 4 carbon atoms or a dihydroxyalkyl of 3 or 4 carbon atoms, when Z is methyl, Cl or Br; or when Z is CH2 OH or a perfluoroalkyl, Ra denotes hydrogen, a monohydroxyalkyl of 2 to 4 carbon atoms or a dihydroxyalkyl of 3 or 4 carbon atoms, and Rb represents 2-hydroxyethyl or 2,3-dihydroxypropyl.
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- 1-[(Heterocyclyl)-alkyl]-4-diarylmethoxy piperidine derivatives
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Novel 1-[(heterocyclyl)alkyl]-4-diarylmethoxy piperidine derivatives are disclosed having the formula STR1 where n is 2-6, Ar1 and Ar2 are aryl and B is a substituted benzimidazolyl radical. These compounds are useful for their antianaphylactic and antihistaminic properties. Specific claimed compounds are 1-{3-[4-(diphenylmethoxy)-1-piperidinyl]-propyl}-1,3-dihydro-2H-benzimidazol-2-one, 1-{2-[4-(diphenylmethoxy)-1-piperidinyl]ethyl}1-, 3-dihydro-2H-benzimidazol-2-one, and 1-{4-[4-(diphenylmethoxy)-1-piperidinyl]butyl}-1,3-dihydro-2H-benzimidazol-2-one.
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- Chemotherapeutically active nitro compounds. I. Nitroanilines
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More than 200 nitro compounds, most of them nitroaniline derivatives substituted with one or more radicals having a basic reaction, were prepared and investigated as to their therapeutic activity against bacteria, fungi, protozoa, helminths, viruses and tumors. Several mono nitrobenzenes with a radical having a basic reaction showed a weak in vitro activity against gram positive bacteria and against Crocker's sarcoma 180; they also showed systemic activity against nematodes (Aspiculuris tetraptera) and viruses. The majority of therapeutically active compounds with pronounced in vitro activity against Trichomonas fetus, Entamoeba histolytica, Schistosoma mansoni, cestodes, nematodes (Ancylostoma caninum), viruses (influenza, MHV, SAV and EMC) and various types of carcinoma (Ehrlich's carcinoma, leukemia 1210, Crocker's sarcoma 180) were dinitrobenzene derivatives with one radical having a basic reaction and electropositive groups or unreactive or reactive chlorine atom, and di nitrobenzene with two equal or two different radicals having a basic reaction. Compound No. 70 revealed a marked in vitro activity against fungi (Trichophyton; Microsporum, Candida albicans). Other nitro compounds such as bis mono and bis dinitrobenzene derivatives likewise showed a systemic action against E. histolytica, viruses and, in particular, carcinoma (Crocker's sarcoma 180, Ridgway's osteosarcoma). Oxygen and sulfur analogue compounds as well as compounds produced by reduction also possessed a distinct activity against E. histolytica and viruses. On the basis of the present results, the dinitrobenzenes substituted with two radicals having a basic reaction include a number which have in common a recognizable structure/activity relationship in respect to E. histolytica, Schistosoma mansoni and different types of viruses. The activity against viruses in this class of compounds is probably due to an increased interferon production in the host animal. Whether the mechanism of action is the same against E. histolytica or Schistosoma mansoni has not been determined so far. A tumorigenic effect was observed mainly in those di nitrobenzenes which are classed as alkylating compounds. Because of the small chemotherapeutic index, the trials were not continued with the most effective compounds mentioned.
- Winkelmann,Raether,Dittmar,et al.
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p. 681 - 708
(2007/10/05)
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