- The Base-Promoted Annulation of 2-Hydrazinyl Pyridine and CO2 toward Triazolones
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A base-promoted annulation of 2-hydrazinyl pyridine and atmospheric pressure of CO2 has been developed in the presence of silane as reducing reagent, affording a series of triazolones in moderate to excellent yields. CO2 served as a carbonyl source in this transfomation. Moreover, benzamidrazones also worked well under this procedure. Thus, it represents a green, sustainable and straightforward pathway to access triazolone frameworks. (Figure presented.).
- Wu, Xiaopeng,Sun, Song,Wang, Bingbing,Cheng, Jiang
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supporting information
p. 3855 - 3859
(2017/11/15)
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- Solvent-promoted catalyst-free: N -formylation of amines using carbon dioxide under ambient conditions
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An unprecedented catalyst-free formylation of amines using CO2 and hydrosilanes was developed. The solvent plays a vital role in promoting the interaction of amines with hydrosilanes and subsequent CO2 insertion, thus facilitating the simultaneous activation of N-H and Si-H bonds. Based on relevant mechanistic studies, a plausible mechanism involving a silyl carbamate intermediate is proposed.
- Lv, Hui,Xing, Qi,Yue, Chengtao,Lei, Ziqiang,Li, Fuwei
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supporting information
p. 6545 - 6548
(2016/06/01)
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- An eco-benign and highly efficient procedure for N-acylation catalyzed by heteropolyanion-based ionic liquids using carboxylic acid under solvent-free conditions
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An eco-benign and highly efficient route for N-acylation of amines has been developed by treating amines with corresponding carboxylic acids in the presence of 2 mol % of heteropolyanion-based ionic liquids as catalysts under solvent-free conditions. This practical reaction could tolerate a wide range of substrates. Thus, various N-acylation products including N-acyl α-amino acid derivatives were obtained in moderate to excellent yields at 70 C to 120 C. Moreover, recycling studies revealed that heteropolyanion-based ionic liquids were easily reusable for this N-acylation. This method provides a green and much improved protocol over the existing methods.
- Chen, Zhikai,Fu, Renzhong,Chai, Wen,Zheng, Hao,Sun, Lin,Lu, Qiang,Yuan, Rongxin
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p. 2237 - 2245
(2014/03/21)
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- 6-Heteroarylpyridoindolone Derivatives, Their Preparation and Therapeutic Use Thereof
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The disclosure relates to compounds of formula (I): wherein R1, R2, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and therapeutic use thereof.
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Page/Page column 13
(2008/12/04)
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- N-PHENYL-1,1,1-TRIFLUOROMETHANESULFONAMIDE HYDRAZONE DERIVATIVE COMPOUNDS AND THEIR USAGE IN CONTROLLING PARASITES
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Novel N-phenyl-1,1,1-trifluoromethanesulfonamide compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo and ex vivo.
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Page/Page column 37
(2008/06/13)
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- Piperazine derivatives as therapeutic agents
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Substituted piperazine compounds of formula I STR1 in which HET is a substituted pyrazole, imidazole or 1,2,4-triazole have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.
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- Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.
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Human beta3 adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over beta1 and beta2 binding. L-760,087 (4a) and L-764,646 (5a) (beta3 EC50 = 18 and 14 nM, respectively) stimula
- Parmee,Naylor,Perkins,Colandrea,Ok,Candelore,Cascieri,Deng,Feeney,Forrest,Hom,MacIntyre,Miller,Stearns,Strader,Tota,Wyvratt,Fisher,Weber
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p. 749 - 754
(2007/10/03)
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- Ethanolic or aqueous formic acid (1:1) - A new efficient reagent for the regeneration of ketones from phenylhydrazones
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50% Ethanolic or aqueous formic acid has been found to be extremely efficacious for the regeneration of aliphatic and aromatic ketones from phenylhydrazones.
- Chakrabarty, Manas,Khasnobis, Shampa
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p. 1361 - 1368
(2007/10/03)
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- Preparation, properties, and reductive alkylation of arylhydrazides
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1 [-Acy]-2-arylhydrazines (1), readily obtained in high yield from the condensation of arylhydrazines and the appropriate liquid carboxylic acid (2), underwent reductive alkylation with the same or different liquid carboxylic acids (2) and NaBH4 to give 1-acyl-2-alkyl-2-arylhydrazines (3) in good to moderate yields. The carboxylic acid has both the role of supplying the entering alkyl group and of acting as solvent. Most likely, it also modifies the BH4- anion to an active reducing agent under those conditions. The 1H NMR criteria for identifying the location of acylation of hydrazines and E and Z isomers are given. The MS spectra of the prepared hydrazides were analyzed in order to identify relevant structural features leading to specific fragmentations.
- Verardo, Giancarlo,Toniutti, Nicoletta,Giumanini, Angelo G.
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p. 1180 - 1187
(2007/10/03)
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- Reduction of Ag(I) by 1-acyl-2-arylhydrazines: Mechanism of photographic infectious development
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The photographic process of 'infectious development' in which 1-acyl-2-arylhydrazines reduce Ag(I) has been studied using analogues. 1-Acyl-2-aryldiazenes, resulting from oxidation of 1-acyl-2-arylhydrazines, are hydrolysed to anions of aryldiazenes (ArN = NH), which undergo further oxidation with loss of nitrogen to yield aryl radicals. The aryl radicals cause 'feedback inhibition' which is prevented by the addition of benzhydrol.
- Bowman, W. Russell,Forshaw, J. Anthony,Hall, Kevin P.,Kitchin, Jonathan P.,Mott, Andrew W.
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p. 3961 - 3972
(2007/10/03)
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