- Copper-catalyzed one-pot synthesis of 1,2,4-triazoles from nitriles and hydroxylamine
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A simple and efficient copper-catalyzed one-pot synthesis of substituted 1,2,4-triazoles through reactions of two nitriles with hydroxylamine has been developed. The protocol uses simple and readily available nitriles and hydroxylamine hydrochloride as th
- Xu, Hao,Ma, Shuang,Xu, Yuanqing,Bian, Longxiang,Ding, Tao,Fang, Xiaomin,Zhang, Wenkai,Ren, Yanrong
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supporting information
p. 1789 - 1794
(2015/02/19)
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- One-Pot Synthesis of N-Monosubstituted Ureas from Nitriles via Tiemann Rearrangement
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Amidoximes, obtained from the reaction of nitriles with hydroxylamine, underwent Tiemann rearrangement in the presence of benzenesulfonyl chlorides (TsCl or o-NsCl) to form the N-substituted cyanamides. Subsequently, acidic hydrolysis of the cyanamides afforded the corresponding N-monosubstituted ureas. The synthesis of N-monosubstituted ureas from nitriles was accomplished by three steps in one pot, which provides a direct access to versatile N-monosubstituted urea derivatives from a wide variety of nitriles.
- Wang, Chien-Hong,Hsieh, Tsung-Han,Lin, Chia-Chi,Yeh, Wen-Hsiung,Lin, Chih-An,Chien, Tun-Cheng
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supporting information
p. 1823 - 1826
(2015/08/06)
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- OXADIAZOLE COMPOUNDS
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The present invention relates to a compound of formula (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein R1,R2,R3,L1,L2,L3,L4,L5 and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.
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Page/Page column 145; 146
(2015/11/11)
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- Practical synthesis of N -substituted cyanamides via tiemann rearrangement of amidoximes
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A facile and general synthesis of various N-substituted cyanamides was accomplished by the Tiemann rearrangement of amidoximes with benzenesulfonyl chlorides (TsCl or o-NsCl) and DIPEA.
- Lin, Chia-Chi,Hsieh, Tsung-Han,Liao, Pen-Yuan,Liao, Zhen-Yuan,Chang, Chih-Wei,Shih, Yu-Chiao,Yeh, Wen-Hsiung,Chien, Tun-Cheng
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supporting information
p. 892 - 895
(2014/03/21)
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- Synthesis and methemoglobinemia-inducing properties of benzocaine isosteres designed as humane rodenticides
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A number of isosteres (oxadiazoles, thiadiazoles, tetrazoles and diazines) of benzocaine were prepared and evaluated for their capacity to induce methemoglobinemia - with a view to their possible application as humane pest control agents. It was found that an optimal lipophilicity for the formation of methemoglobin (metHb) in vitro existed within each series, with 1,2,4-oxadiazole 3 (metHb% = 61.0 ± 3.6) and 1,3,4-oxadiazole 10 (metHb% = 52.4 ± 0.9) demonstrating the greatest activity. Of the 5 candidates (compounds 3, 10, 11, 13 and 23) evaluated in vivo, failure to induce a lethal end-point at doses of 120 mg/kg was observed in all cases. Inadequate metabolic stability, particularly towards hepatic enzymes such as the CYPs, was postulated as one reason for their failure.
- Conole, Daniel,Beck, Thorsten M.,Jay-Smith, Morgan,Tingle, Malcolm D.,Eason, Charles T.,Brimble, Margaret A.,Rennison, David
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supporting information
p. 2220 - 2235
(2014/04/17)
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- Synthesis of amidoximes using an efficient and rapid ultrasound method
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This is a report on an efficient and rapid synthesis of amidoximes using ultrasound irradiation with appropriate nitrile and hydroxylamine hydrochloride in water/ethanol. This new synthetic methodology is compared with previously known methods. The main a
- Barros, Carlos Jonnatan Pimentel,De Freitas, Jucleiton J. Rufino,De Oliveira, Ronaldo N.,De Freitas Filho, Jo?o R.
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experimental part
p. 721 - 722
(2012/05/20)
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- Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119
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GPR119 is a rhodopsin-like GPCR expressed in pancreatic β-cells and incretin releasing cells in the GI tract. As with incretins, GPR119 increases cAMP levels in these cell types, thus making it a highly attractive potential target for the treatment of dia
- Semple, Graeme,Fioravanti, Beatriz,Pereira, Guillherme,Calderon, Imelda,Uy, Jane,Choi, Karoline,Xiong, Yifeng,Ren, Albert,Morgan, Michael,Dave, Vibha,Thomsen, William,Unett, David J.,Xing, Charles,Bossie, Stuart,Carroll, Chris,Chu, Zhi-Liang,Grottick, Andrew J.,Hauser, Erin K.,Leonard, James,Jones, Robert M.
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scheme or table
p. 5172 - 5175
(2009/07/01)
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- PYRAZOLO [1,5-ALPHA] PYRIMIDINYL DERIVATIVES USEFUL AS CORTICOTROPIN-RELEASING FACTOR (CRF) RECEPTOR ANTAGONISTS
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CRF receptor antagonists are disclosed which may have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in mammals. The CRF receptor antagonists of this invention have the following structure: (I); and pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof, wherein R1, R2a, R2b, Y, Het, n, o, R6, Ar and R7 are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
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Page/Page column 49
(2008/06/13)
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- HETEROCYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
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Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, V R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
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Page/Page column 46
(2010/10/20)
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- ORGANIC COMPOUNDS
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Compounds of Formula (I); in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
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Page/Page column 34
(2008/06/13)
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- Syntheses of 2-(bromodifluoromethyl)benzoxazole and 5-(bromodifluoromethyl)-1,2,4-oxadiazoles
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Facile syntheses of CF2Br-substituted heterocycles are reported. Preparation of 2-(bromodifluoromethyl)benzoxazole (2) was achieved in two steps by reaction of 2-aminophenol (3) with CF2BrCO2Et to give amide (4), followed by cyclization of 4 with PPA to give 2. The 5-(bromodifluoromethyl)-1,2,4-oxadiazoles (6a-c) were prepared by one step reaction of amidoximes (5a-c) with CF2BrCO2Et. These CF2Br-substituted heterocycles are intermediates in an ongoing investigation of the synthesis of inhibitors of HIV reverse transcriptase having a CF2 substitution.
- Dolbier Jr., William R.,Burkholder, Conrad R.,Medebielle, Maurice
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p. 127 - 130
(2007/10/03)
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- The Syntheses of Triazole, Sulfur-Containing Diazole and N-Phenylthiatriazole Biphenyltetrazoles as Potential Angiotensin II Receptor Antagonists
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The syntheses of triazole, sulfur-containing diazole and N-phenylthiatriazole analogs of imidazole angiotensin II antagonist, DuP 753, are reported. 5-Butyl-3-[(2-trifluoromethyl)phenyl]-2,1,3,4-1H-thiatriazole-2-one biphenyltetrazole (63) is found to hav
- Chou, Shan-Yen,Chen, Su-San,Ho, Chin-Chung,Huang, Shiang-Ling,Huang, Tsai-Mien,Pan, Ohm-Guo,Wang, Chia-Lin,Chen, Ying,Lu, Hsiao-Hwa,Liu, Shih-Hwa,Huang, Shir-Ly,Chiang, Ren-Shou
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- PRODRUGS OF IMIDAZOLE CARBOXYLIC ACIDS AS ANGIOTENSIN II RECEPTOR ANTAGONISTS
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Prodrugs of imidazole carboxylic acids which are AII antagonists useful in treating hypertension, pharmaceutical compositions thereof and a method of treating hypertension using such prodrugs are disclosed.
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