- A new stereoselective synthesis of 2-amino-4,5-dihydrothiophene-3- carbonitrile derivatives
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A new stereoselective method for the synthesis of trans-isomers of 2-amino-4-aryl-5-benzoyl-4,5-dihydrothiophene-3-carbonitriles was proposed. The method involves base-catalyzed reactions of phenacyl thiocyanate with 3-(het)aryl-2-cyanoprop-2-enethioamides. (4R,5S/4S,5R)-2-Amino-5-benzoyl-4-(2- chlorophenyl)-4,5-ihydrothiophene-3-carbonitrile was structurally characterized by X-ray diffraction analysis.
- Dotsenko,Krivokolysko,Chernega,Litvinov
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Read Online
- Panchromatic Push-Pull Chromophores based on Triphenylamine as Donors for Molecular Solar Cells
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Two new push-pull chromophores based on triphenylamine as donor and 2-carboxymethyl-2-cyanomethylenethiazole as acceptor have been synthesized. Both exhibit strong light absorption covering from 300 to 800 nm. Electrochemical studies show HOMO-LUMO gaps o
- Esteban, Sandra Gomez,De La Cruz, Pilar,Aljarilla, Ana,Arellano, Luis M.,Langa, Fernando
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Read Online
- Diiiodine/Potassium Persulfate Mediated Synthesis of 1,2,3-Thiadiazoles from N -Tosylhydrazones and a Thiocyanate Salt as a Sulfur Source under Transition-Metal-Free Conditions
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A highly efficient method for the synthesis of 1,2,3-thiadiazoles has been developed by utilizing readily available tosylhydrazones and ammonium thiocyanate with ecofriendly EtOH as the solvent at room temperature. The reaction shows a wide scope of subst
- Lu, Yuhan,Sun, Yadong,Abdukader, Ablimit,Liu, Chenjiang
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supporting information
p. 1044 - 1048
(2021/05/05)
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- α-Selective C(sp3)-H Thio/Selenocyanation of Ketones with Elemental Chalcogen
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A facile method is disclosed for the synthesis of α-thio/selenocyanato ketones through regioselective C-H thio/selenocyanation of ketones. The advantages include the use of easily available starting materials, high efficiency, simple operation, and easy scale-up. Control experiments provide evidence that the reaction proceeded via a radical way, while kinetic isotope effect experiments reveal that the cleavage of the C-H bond serves as the rate-limiting step.
- Li, Jin-Cheng,Gao, Wen-Xia,Liu, Miao-Chang,Zhou, Yun-Bing,Wu, Hua-Yue
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p. 17294 - 17306
(2021/12/02)
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- Visible-light-promoted thiocyanation of sp2C-H bonds over heterogeneous graphitic carbon nitrides
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Mesoporous graphitic carbon nitride (mpg-C3N4) has been developed as a metal-free heterogeneous photocatalyst for thiocyanation transformations. The reaction proceeds efficiently by utilizing air as a green oxidant under mild reaction conditions, which affords SCN-containing compounds in moderate to excellent yields. Meanwhile, the practicality of this protocol is further demonstrated by the reusability of the mpg-C3N4photocatalyst and the scaled-up reaction. Furthermore, detailed mechanistic studies clearly demonstrate the role of oxygen.
- Chen, Wei,Li, Tingzhen,Peng, Xinwen
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supporting information
p. 14058 - 14062
(2021/08/16)
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- Boron-doped TiO2(B-TiO2): visible-light photocatalytic difunctionalization of alkenes and alkynes
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Boron-doped TiO2(B-TiO2) was prepared, characterized, and successfully applied as a reusable, inexpensive, available, and heterogeneous nanophotocatalyst under visible light for a novel method of construction of phenacyl thiocyanate compounds from double or triple bonds. Impressive aspects of this project are obtaining the desired compounds in a short time, using a renewable energy source, and using a catalyst with easy extraction that is solvent-safe, and without the use of any oxidants, bases, and ligands, or harsh conditions. This is the first report of the construction of phenacyl thiocyanates through this photocatalytic method under visible light.
- Hosseini-Sarvari, Mona,Valikhani, Atefe
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supporting information
p. 12464 - 12470
(2021/07/25)
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- Visible-Light-Mediated Additive-Free Decarboxylative Ketonization Reaction of Acrylic Acids: An Access to α-Thiocyanate Ketones
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Visible-light-mediated additive-free decarboxylative functionalization of acrylic acids has been developed. The reaction uses inexpensive organic dye 9,10-dicyanoanthracene as a photocatalyst and uses the ubiquitous dioxygen as both an oxygen source and an oxidant. Through this mild and environmentally friendly method, a series of important α-thiocyanate ketones can be generated from easily available acrylic acids and ammonium thiocyanate. In addition, the facile transformation of product α-thiocyanate ketones makes this method have great potential for application in organic and pharmaceutical chemistry.
- Wang, Zhi-Lv,Chen, Jie,He, Yan-Hong,Guan, Zhi
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supporting information
p. 3741 - 3749
(2021/03/09)
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- Thiocyanation and 2-Amino-1,3-thiazole Formation in Water Using Recoverable and Reusable Glycosylated Resorcin[4]arene Cavitands
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A family of three spatially directional resorcin[4]arene cavitand glycoconjugates (RCGs) have been applied as efficient recoverable and reusable inverse phase transfer catalysts for eco- A nd environmentally friendly thiocyanation and 2-amino-1,3-thiazole formation reactions in water. The results show that RCGs (1 mol %) were capable of hosting and catalyzing various water-insoluble bromo/thiocyanato substrates in water without the use of any co-organic solvents. The recoverability and reusability of RCG catalytic systems, that is, RCG1 and RCG3, were also examined upon a simple extraction of the desired products using DCM or ethyl acetate, followed by subjecting the recovered aqueous solution containing the RCG catalysts to the next reaction cycles.
- Husain, Ali A.,Bisht, Kirpal S.
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p. 9928 - 9935
(2020/09/03)
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- Synthesis and Use of Trifluoromethylthiolated Ketenimines
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The synthesis of trifluoromethylthiolated ketenimines is herein described. They are easily synthesized from the corresponding α-trifluoromethylthiolated oximes upon activation with triflic anhydride and a base. The presumed nitrilium ion resulting from the Beckmann rearrangement is deprotonated to lead to the key intermediate, whose stability brought by the fluorinated substituent was unforeseeable. The reaction of these new building blocks with a variety of nucleophiles affords a vast array of cyclic and acyclic products bearing the valuable SCF3 moiety.
- Guérin, Thomas,Pikun, Nadiia V.,Morioka, Ryutaro,Panossian, Armen,Hanquet, Gilles,Leroux, Frédéric R.
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supporting information
p. 14852 - 14855
(2020/10/19)
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- EIF4E INHIBITORS AND USES THEREOF
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The present invention provides compounds inhibiting elF4E activity, and compositions and methods of using thereof. Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful for treating a variety of diseases, dis
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Paragraph 00313
(2020/03/29)
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- TMSCl-Catalyzed Electrophilic Thiocyano Oxyfunctionalization of Alkenes Using N-Thiocyano-dibenzenesulfonimide
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Numerous electrophilic thiocyano oxyfunctionalization reactions of alkenes have been achieved using N-thiocyano-dibenzenesulfonimide, which is a new electrophilic thiocyanation reagent and could be easily prepared in two steps from dibenzenesulfonimide. T
- Ye, Ai-Hui,Zhang, Ye,Xie, Yu-Yang,Luo, Hui-Yun,Dong, Jia-Wei,Liu, Xiao-Dong,Song, Xu-Feng,Ding, Tongmei,Chen, Zhi-Min
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supporting information
p. 5106 - 5110
(2019/09/03)
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- I2/CuCl2-promoted one-pot three-component synthesis of aliphatic or aromatic substituted 1,2,3-thiadiazoles
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An efficient I2/CuCl2-promoted one-pot three-component strategy for the construction of 1,2,3-thiadiazoles from aliphatic- or aromatic-substituted methyl ketones, p-toluenesulfonyl hydrazide, and potassium thiocyanate has been develo
- Wang, Can,Geng, Xiao,Zhao, Peng,Zhou, You,Wu, Yan-Dong,Cui, Yan-Fang,Wu, An-Xin
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supporting information
p. 8134 - 8137
(2019/07/15)
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- Imidazolium-Based Ionic Network as a Robust Heterogeneous Catalyst in Synthesis of Phenacyl Derivatives
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A new imidazolium-based poly(ionic liquid) has been synthesized and used as a robust heterogeneous catalyst for the preparation of phenacyl derivatives by an SN2 reaction of different phenacyl bromides with a broad range of nucleophiles. The products are obtained in high yields under mild conditions. The catalyst can be recycled efficiently.
- Kakesh,Sayyahi,Badri,Tahanpesar
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p. 1218 - 1220
(2019/07/16)
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- Photo-sensitized oxy-thiocyanation of terminal alkynes/1,3-aryldienes and their one-pot conversion to 2-hydroxy 4-substituted aryl thiazoles
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A regioselective visible light induced synthesis of aryl α-thiocyano ketones/thiocyano alcohols from activated terminal aryl alkynes and aryl 1,3-conjugated dienes was achieved. This mild and non-metallic oxidation is exclusively driven by benign ambient air in the presence of an organic photo-catalyst and NH4SCN. This protocol was also demonstrated at the 5 mmol scale for the synthesis of potentially therapeutic 2-hydroxy 4-substituted arylthiazoles in good yields, signifying its amenability for large-scale application.
- Gullapalli, Kumaraswamy,Vijaykumar, Swargam
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p. 2232 - 2241
(2019/02/27)
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- Visible-Light-Promoted Difunctionalization of Olefins Leading to α-Thiocyanato Ketones
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A simple and convenient visible-light-induced difunctionalization of alkenes with ammonium thiocyanate and dioxygen has been developed at room temperature. A series of α-thiocyanato ketones could be easily and efficiently obtained in moderate to good yields through the formation of C-S and C=O bonds simply by using nontoxic and inexpensive Na 2 -Eosin Y as a photocatalyst.
- Nan, Guangming,Yue, Huilan
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supporting information
p. 1340 - 1345
(2018/05/03)
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- Ammonium [11C]thiocyanate: revised preparation and reactivity studies of a versatile nucleophile for carbon-11 radiolabelling
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Herein we report the preparation of ammonium [11C]thiocyanate via the reaction of [11C]CS2 with ammonia. The [11C]SCN- ion is demonstrated as a potent nucleophile that can be used to readily generate a range of 11C-labelled thiocyanate molecules in high conversions. Furthermore, novel 11C-labelled thiazolone molecules can be easily prepared from the intermediate α-thiocyanatophenones via an acid mediated cyclisation reaction.
- Haywood, Tom,Cesarec, Sara,Kealey, Steven,Plisson, Christophe,Miller, Philip W.
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supporting information
p. 1311 - 1314
(2018/08/28)
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- Ag-Catalyzed Thiocyanofunctionalization of Terminal Alkynes to Access Alkynylthiocyanates and α-Thiocyanoketones
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Unprecedented one-pot thiocyanofunctionalizations of terminal alkynes to deliver alkynylthiocyanates and α-thiocyanoketones using a silver-catalyzed procedure or under silver/gold relay catalysis is reported. These synthetically valuable organothiocyanates are accessed in high efficiency, and their derivatization into a variety of valuable sulfur-containing heterocycles and sulfides has also been demonstrated.
- See, Jie Yang,Zhao, Yu
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supporting information
p. 7433 - 7436
(2018/12/11)
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- Redox Active Sodium Iodide/Recyclable Heterogeneous Solid Acid: An Efficient Dual Catalytic System for Electrochemically Oxidative α-C?H Thiocyanation and Sulfenylation of Ketones
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An efficient electrochemically oxidative α-C?H thiocyanation and sulfenylation of ketones has been developed in a simple undivided cell under constant current condition.?The electrochemistry performs using NaI as the redox catalyst and heterogeneous solid salt Amberlyst-15(H) (A-15(H)) as proton catalyst?without the addition of external conductive salts. The protocol proved to be practical since the solid salt could be reused in up to five consecutive gram-scale runs without significant decrease in efficiency. Control experiments and cyclic voltammetry analysis disclose that the reaction proceeds likely via a cascade α-halogenation and subsequent thiocyanation or sulfenylation. (Figure presented.).
- Liang, Sen,Zeng, Cheng-Chu,Tian, Hong-Yu,Sun, Bao-Guo,Luo, Xu-Gang,Ren, Fa-Zheng
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p. 1444 - 1452
(2017/12/18)
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- Allosteric Inhibitors of SHP2 with Therapeutic Potential for Cancer Treatment
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SHP2, a cytoplasmic protein-tyrosine phosphatase encoded by the PTPN11 gene, is involved in multiple cell signaling processes including Ras/MAPK and Hippo/YAP pathways. SHP2 has been shown to contribute to the progression of a number of cancer types inclu
- Xie, Jingjing,Si, Xiaojia,Gu, Shoulai,Wang, Mingliang,Shen, Jian,Li, Haoyan,Li, Dan,Fang, Yanjia,Liu, Cong,Zhu, Jidong
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p. 10205 - 10219
(2018/01/10)
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- One-pot synthesis of (ethoxycarbonyl)difluoromethylthioethers from thiocyanate sodium and ethyl 2-(trimethylsilyl)-2,2-difluoroacetate (TMS-CF2CO2Et)
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An efficient one-pot cascade methodology for the synthesis of (ethoxycarbonyl)difluoromethyl thioethers is described. Benzyl, allyl, alkyl halides or diazonium salts as the starting materials together with thiocyanate sodium and TMS-CF2CO2Et in the presence of CsF or NaOAc afford a variety of the fluoroalkylthiolated products in moderate to good yields.
- Xu, Lijun,Wang, Hongyu,Zheng, Changwu,Zhao, Gang
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supporting information
p. 6057 - 6066
(2017/09/23)
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- Graphene oxide: A promising carbocatalyst for the regioselective thiocyanation of aromatic amines, phenols, anisols and enolizable ketones by hydrogen peroxide/KSCN in water
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Graphene oxide (GO), as a heterogeneous carbocatalyst, catalyzes the direct thiocyanation of a variety of arenes including aromatic amines, phenols, anisols and carbonyl compounds that possessing α-hydrogen in the presence of hydrogen peroxide and KSCN in water as a green media. This procedure is chemoselective, avoids the use of precious metals and toxic solvents and has a broad substrate scope. Easy removal from the reaction mixture and recyclability with no loss of activity are the key features of graphene oxide in this catalytic system.
- Khalili, Dariush
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p. 2547 - 2553
(2016/03/19)
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- Integration of aqueous biphasic with magnetically recyclable systems: Polyethylene glycol-grafted Fe3O4 nanoparticles catalyzed phenacyl synthesis in water
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The present work trends to define an efficient phenacyl catalytic synthesis method employing a new nano-magnetite-supported organocatalyst. Polyethylene glycol (PEG) was bonded successfully onto silica coated ferrite and the resultant nanoparticles (PEG@SiO2@Fe3O4) characterized by fourier transform infrared spectroscopy (FT-IR), atomic force microscopy (AFM), thermal gravimetric analysis (TGA), vibrating sample magnetometry (VSM), energy dispersive X-ray analysis (EDAX) and X-ray diffraction (XRD) that exhibited a good catalytic activity in the reaction. The nanoparticles could be easily separated from the reaction mixture by an external magnet and reused in seven reaction cycles without significant loss of activity.
- Amini, Atefeh,Sayyahi, Soheil,Saghanezhad, Seyyed Jafar,Taheri, Narges
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- Oxidant-free thiocyanation of phenols and carbonyl compounds under solvent-free conditions by AlCl 3/NH 4SCN
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A simple, efficient, solvent-free, and mild method for thiocyanation of phenols by ammonium thiocyanate (NH4SCN) in the presence of AlCl3 has been developed. This new methodology was used to prepare para-thiocyanated products in good to excellent yields at 70°C. In addition, the successful α-thiocyanation of various ketones has also been described. Finally, a plausible mechanism of thiocyanation has been suggested.
- Nikoofar, Kobra,Gorji, Samareh
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- A 2-thiocyano HYPNONE derivatives method for the preparation of
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The invention discloses a method for preparing 2-sulfur cyano acetophenone derivatives. The method for preparing the 2-sulfur cyano acetophenone derivatives comprises the following steps: dissolving styrene derivatives and ammonium thiocyanate in a solvent, and reacting at 20-30 DEG C to obtain 2-sulfur cyano acetophenone derivatives. According to the method for preparing the 2-sulfur cyano acetophenone derivatives, the styrene derivatives are taken as starting materials; the raw materials are easily available and various in type; products prepared by the method have various in type, can be directly used and can also be used for other further reactions; meanwhile, the method is mild in reaction conditions and simple in reaction operation and post-processing process; an accelerant does not need to be added; the production process meets the green and chemical requirements, is relatively high in yield and is suitable for large-scale production.
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Paragraph 0032-0035
(2016/10/10)
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- COMPOUNDS AND METHODS for the inhibition of HDAC
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Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
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Paragraph 0694-0695
(2015/11/24)
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- Solvent-free synthesis of novel (E)-2-(3,5-dimethyl-4-(aryldiazenyl)-1H-pyrazol-1-yl)-4-arylthiazoles: Determination of their biological activity
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In search of novel biologically active azoles, some new (E)-2-(3,5-dimethyl-4-(aryldiazenyl)-1H-pyrazol-1-yl)-4-arylthiazoles 3a-p have been synthesized via Hantzsch thiazole approach under greener, mild and solvent-free conditions. Structures of all comp
- Kaur, Kamalneet,Kumar, Vinod,Beniwal, Vikas,Kumar, Vikas,Aneja,Sharma, Vishal,Jaglan, Sundeep
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p. 3863 - 3875
(2015/10/06)
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- One-pot anodic thiocyanation and isothiocyanation of alkenes
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The one-pot anodic thiocyanation and isothiocyanation of alkenes in both acidic two-phase (water-dichloromethane) and homogeneous one-phase (water-acetonitrile) media has been studied. Optimisation experiments on tetramethylethylene as a model alkene invo
- Levy, Avishai,Becker, James Y.
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p. 294 - 302
(2015/08/24)
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- Molecular oxygen induced free radical oxythiocyanation of styrenes leading to α-oxothiocyanates
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A facile and efficient protocol of oxythiocyanation of styrenes with ammonium thiocyanate has been developed. The reaction proceeded at room temperature using oxygen as sole oxidant to afford the α-oxothiocyanates via radical pathway in moderate to good yields. This method is straightforward, green and cost-effective, requires no catalyst and additives.
- Liu, Kui,Li, Da-Peng,Zhou, Shao-Fang,Pan, Xiang-Qiang,Shoberu, Adedamola,Zou, Jian-Ping
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supporting information
p. 4031 - 4034
(2015/06/02)
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- Ambient benzotriazole ring opening through intermolecular radical addition to vinyltriazole
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Radical addition to vinyltriazole was developed as a new approach to achieve 1,2,3-triazole ring opening under mild conditions. Through reagent control, excellent chemoselectivity was achieved, giving either nitrile under basic conditions or quinoxaline under neutral conditions. Reactivities made this method an attractive new reaction mode.
- Su, Yijin,Petersen, Jeffrey L.,Gregg, Tesia L.,Shi, Xiaodong
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supporting information
p. 1208 - 1211
(2015/03/14)
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- SUBSTITUTED DIARYL AZETIDINE DERIVATIVES AS SPHINGOSINE RECEPTOR MODULATORS
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The present invention relates to substituted diaryl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
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Paragraph 0280; 0281; 0282
(2014/09/03)
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- SUBSTITUTED DIARYL DERIVATIVES AS SPHINGOSINE RECEPTOR MODULATORS
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The present invention relates to substituted diaryl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
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Paragraph 0115; 0116; 0117
(2014/09/03)
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- Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors
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A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the l
- Kono, Mitsunori,Matsumoto, Takahiro,Kawamura, Toru,Nishimura, Atsushi,Kiyota, Yoshihiro,Oki, Hideyuki,Miyazaki, Junichi,Igaki, Shigeru,Behnke, Craig A.,Shimojo, Masato,Kori, Masakuni
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- β-cyclodextrin immobilized onto dowex resin: A unique microvessel and heterogeneous catalyst in nucleophilic substitution reactions
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The catalytic activity of β-cyclodextrin immobilized on Dowex resin as an efficient solid-liquid phase transfer catalyst was developed for the synthesis of alkyl thiocyanates and phenacyl derivatives in water. The nucleophilic substitution reactions were performed under mild reaction condition and gave the products in excellent yields. Furthermore, the catalyst could be recycled by facile separation without any loss of activity.
- Kiasat, Ali Reza,Zarinderakht, Nasrollah,Sayyahi, Soheil
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experimental part
p. 699 - 702
(2012/05/05)
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- A convenient, rapid, and general synthesis of α-oxo thiocyanates using clay supported ammonium thiocyanate
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A very rapid, convenient, and general method for the synthesis of α-oxo thiocyanates has been described by using clay supported ammonium thiocyanate. The procedure avoids the use of additional catalyst, solvent, aqueous work-up and the yields are high. Moreover, the method is applicable for a variety of aryl, heteroaryl, alkyl α-halo carbonyls, β-keto tosylates, α-halo β-dicarbonyl, α-tosyl, β-dicarbonyl, alkyl halide, and alkyl tosylates.
- Meshram,Thakur, Pramod B.,Madhu Babu,Bangade, Vikas M.
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experimental part
p. 1780 - 1785
(2012/05/04)
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- Inhibitory effect of 4-aryl 2-substituted aniline-thiazole analogs on growth of human prostate cancer LNCap cells
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Androgen receptor (AR) is ligand-inducible nuclear hormone receptor which has been focused on key molecular target in growth and progression of prostate cancer. We synthesized a series of 4-aryl 2-substituted aniline-thiazole analogs and evaluated their anti-cancer activity in AR-dependent human prostate cancer LNCap cells. Among them, the compound 6 inhibited the tumor growth in LNCap-inoculated xenograft model.
- Baek, Seung-Hwa,Kim, Nakjeong,Kim, Seong Hwan,Park, Kwang Hwa,Jeong, Kyung-Chae,Park, Bae Keun,Kang, Nam Sook
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scheme or table
p. 111 - 114
(2012/03/26)
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- Efficient α-thiocyanation of ketones using pyridinium hydrobromide perbromide
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The direct α-thiocyanation of ketones with ammonium thiocyanate has been achieved using pyridinium hydrobromide perbromide under mild and neutral conditions to produce α-ketothiocyanates in excellent yields and with high selectivity. Copyright
- Wu, Liqiang,Yang, Xiaojuan
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experimental part
p. 748 - 753
(2012/06/18)
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- Selectfluor: A novel and efficient reagent for the rapid α-thiocyanation of ketones
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The direct α-thiocyanation of ketones with ammonium thiocyanate has been achieved using Selectfluor under mild and neutral conditions to produce α-ketothiocyanates, in excellent yields and with high selectivity.
- Wu, Dezhen,Yang, Xiaojuan,Wu, Liqiang
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p. 901 - 905,5
(2020/09/09)
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- Convenient and simple synthesis of 2-aminothiazoles by the reaction of α-halo ketone carbonyls with ammonium thiocyanate in the presence of N-methylimidazole
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Substituted 2-aminothiazole derivatives were obtained as a result of N-methylimidazole catalyzed cyclization of α-halo ketone carbonyls with ammonium thiocyanate in water-alcoholic media. The generality of the method has been demonstrated by screening a series of aromatic/heteroaromatic/aliphatic α-halo ketones, α-halo β-diketones, and α-halo β-ketoesters. The developed method is simple, mild, and general route for the preparation of diversely functionalized 2-aminothiazoles in good to moderate yields from readily available starting materials.
- Meshram,Thakur, Pramod B.,Madhu Babu,Bangade, Vikas M.
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p. 5265 - 5269
(2012/10/30)
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- Cis-1,4-bis(triphenylphosphonium)-2-butene peroxodisulfate as an efficient reagent for the synthesis of phenacyl thiocyanates and phenacyl azides
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Styrenes efficiently undergo thiocyanation and azidation with cis-1,4-bis(triphenylphosphonium)-2-butene peroxodisulfate at 0C to furnish the corresponding thiocyanatoketones and azidoketones. This method is a direct, one-pot synthesis under mild condition using methanol as solvent.
- Badri, Rashid,Gorjizadeh, Maryam
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experimental part
p. 2058 - 2066
(2012/06/04)
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- Efficient solution-processed bulk heterojunction solar cells by antiparallel supramolecular arrangement of dipolar donor-acceptor dyes
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A series of dipolar donor-acceptor (D-A) chromophores with aminothiophene donor and different heterocyclic acceptor units is reported. By modulation of the acceptor strength, absorption bands over the whole visible spectrum are accessible as well as adjustment of the frontier molecular orbital levels. The performance of the chromophores in blends with fullerene acceptors in solution-processed bulk heterojunction solar cells was studied and related to the molecular properties of the dyes. In particular, the effect of the large ground-state dipole moments of these dyes was investigated by single crystal X-ray analysis, which revealed antiparallel dimers, resulting in an annihilation of the dipole moments. This specific feature of supramolecular organization explains the excellent performance of merocyanine dyes in organic solar cells. With blends of HB366:PC71BM, the most efficient solar cell with a VOC of 1.0 V, a JSC of 10.2 mAcm-2, and a power-conversion efficiency of 4.5% was achieved under standard AM1.5, 100 mWcm-2 conditions. Under reduced lighting conditions, even higher efficiencies up to 5.1% was obtained. Donor-acceptor dyes with an aminothiophene donor show ideal absorption, redox, and packing features in organic photovoltaics (see picture). With blends of HB366:PC71BM, highly efficient solar cells were achieved with a VOC of 1.0 V, a J SC of 10.2 mAcm-2, and a power conversion efficiency of 4.5%. Copyright
- Buerckstuemmer, Hannah,Tulyakova, Elena V.,Deppisch, Manuela,Lenze, Martin R.,Kronenberg, Nils M.,Gsaenger, Marcel,Stolte, Matthias,Meerholz, Klaus,Wuerthner, Frank
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supporting information; experimental part
p. 11628 - 11632
(2012/01/06)
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- One-pot tandem copper-catalyzed library synthesis of 1-thiazolyl-1,2,3- triazoles as anticancer agents
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One-pot multicomponent synthesis to assemble compounds has been an efficient method for constructing a compound library. We have developed one-pot tandem copper-catalyzed azidation and CuAAC reactions that afford 1-thiazolyl-1,2,3-triazoles with anticancer activity. By utilizing this one-pot synthetic strategy, we constructed a library of 1-thiazolyl-1,2,3-triazoles in search of the potent lead compound. Furthermore, 1-thiazolyl-1,2,3-triazoles were evaluated for anticancer activity against the multidrug-resistant cancer cells MES-SA/Dx5. Most of the 1-thiazolyl-1,2,3-triazoles revealed cytotoxic effect against cancer cells at micromolar to low micromolar range. Testing some of the most potent compounds (5{4,2-4} and 5{5,1-3}) against the normal cell line Vero showed no significant toxicity (except 5{4,2}) to normal cells. This result indicates that compounds 5{4,3-4} and 5{5,1-3} possessed good potency and selectivity to cancer cells over normal cells.
- Li, Wen-Tai,Wu, Wan-Hsun,Tang, Chien-Hsiang,Tai, Ready,Chen, Shui-Tein
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scheme or table
p. 72 - 78
(2011/04/17)
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- An efficient method for synthesis of phenacyl derivatives under homogeneous phase transfer catalyst condition in aqueous media
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In this letter, a mild and efficient procedure for synthesis of phenacyl derivatives under homogenous catalysis in the presence of tetrabutylammonium bromide in aqueous media is described. The nucleophilic substitution reactions were performed under ecofriendly conditions and gave the corresponding products in high yields and short reaction times.
- Sayyahi, Soheil,Saghanezhad, Jafar
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experimental part
p. 300 - 302
(2012/01/14)
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- I2O5 as a mild, inexpensive, and environmentally benign oxidant for the α-thiocyanation of ketones
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-Thiocyanation of various ketones has been achieved using ammonium thiocyanate as a thiocyanation reagent and I2O5 as an oxidant in methanol solution at room temperature. Figure Presented.
- Wu, Liqiang,Yang, Xiaojuan,Yan, Fulin
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experimental part
p. 105 - 110
(2012/01/06)
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- NBS or DEAD as effective reagents in α-thiocyanation of enolizable ketones with ammonium thiocyanate
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Ketones possessing α-hydrogen undergo smooth thiocyanation with ammonium thiocyanate in the presence of N-bromosuccinimide (NBS) at room temperature in acetonitrile under neutral conditions to produce the corresponding α-ketothiocyanates in excellent yiel
- Reddy, B.V. Subba,Reddy, S. Madhu Sudana,Madan, Ch.
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experimental part
p. 1432 - 1435
(2011/06/10)
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- Ionic liquid brush as a highly efficient and reusable catalyst for on-water nucleophilic substitutions
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A very efficient and reusable catalyst has been developed for the on-water nucleophilic substitution of alkyl halides and tosylates with azide or thiocyanate in excellent to quantitative yields. The reaction proceeds smoothly and cleanly without any organic cosolvent or other adductive, and the brush can be reused at least 10 times without noticeable loss of the catalytic activity. The high efficiency, simplicity of product and catalyst isolation, outstanding recyclability, and organic-solvent-free conditions show promise for the use of this catalyst in the laboratory and in industry. A highly efficient and reusable ionic liquid brush catalyst has been developed for the on-water nucleophilic substitution of alkyl halides and tosylates with azide or thiocyanate in excellent to quantitative yields without any organic cosolvent or other adductive. The catalyst can be reused at least 10 times without noticeable loss of the catalytic activity. Copyright
- Li, Jing,Cao, Jing-Jing,Wei, Jun-Fa,Shi, Xian-Ying,Zhang, Li-Hui,Feng, Jin-Juan,Chen, Zhan-Guo
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supporting information; experimental part
p. 229 - 233
(2011/03/20)
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- Mild and efficient method for-thiocyanation of ketones and-dicarbonyl compounds using bromodimethylsulfonium bromide-ammonium thiocyanate
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An efficient and convenient method for-thiocyanation of ketones and-dicarbonyl compounds has been developed using a reagent combination of bromodimethylsulfonium bromide (BDMS) and ammonium thiocyanate in acetonitrile. The developed method is mild and gave good yield of the products at room temperature.
- Bhalerao, Dinesh S.,Akamanchi, Krishnacharya G.
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experimental part
p. 799 - 807
(2010/05/17)
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- A simple and efficient thiocyanation of indoles, anilines and keto compounds catalyzed by a polystyrene resin amberlyst-15
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Thiocyanation of various aromatic, heteroaromatic and enolizable ketone compounds has been achieved with ammonium thiocyanate in presence of polystyrene cation exchange resin, Amberlyst-15. All the reactions were carried out in acetonitrile at room temper
- Lenin, Racha,Raju, Rallabandi M.
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experimental part
p. 392 - 395
(2011/04/12)
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- Heteropoly acids as heterogeneous and reusable catalyst for α-thiocyanation of ketones
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Simple, efficient, and mild method for -thiocyanation of ketones in presence of heteropolyacid has been developed. This methodology offered -oxothiocyanates in good to excellent yields at room temperature in a highly selective manner. The catalyst could b
- Chaskar, Atul C.,Yadav, Arun A.,Langi, Bhushan P.,Murugappan, Anita,Shah, Chetan
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experimental part
p. 2850 - 2856
(2010/10/20)
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- Simple and quick preparation of α-thiocyanate ketones in hydroalcoholic media. Access to 5-aryl-2-imino-1,3-oxathiolanes
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A simple preparation on gram-scale of thiocyanate derivatives via nucleophilic substitution of halogenated compounds with SCN salts at high substrate concentrations in a few minutes and excellent yields was successfully accomplished in hydroalcoholic media. The obtained compounds were employed for the efficient synthesis of valuable 5-aryl-2-imino-1,3-oxathiolane derivatives (a one-pot approach is also presented).
- Bisogno, Fabricio R.,Cuetos, Anibal,Lavandera, Ivan,Gotor, Vicente
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supporting information; experimental part
p. 452 - 454
(2010/04/22)
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- CYCLIC INHIBITORS OF 11β-HYDROXYSTERIOD DEHYDROGENASE 1
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This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih); (Ii); (Ij), (Ik), (II) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
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Page/Page column 184-185
(2009/03/07)
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