- Facile entry into structurally diverse, privileged, (hetero)arene-fused N-alkoxy 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-ones
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Rare and highly medicinally relevant N-alkoxy-substituted benzo[1,4]oxazepines have been synthesized conveniently via the base-promoted SNAr/Smiles rearrangement/SNAr tandem cyclization of N-alkoxysalicylamides with a range of bis-electrophilic substrates; subsequent de-alkylation gives rise to the respective N-hydroxy versions. The compounds reported herein significantly add to the contemporary arsenal of small molecule tools for drug discovery.
- Sapegin, Alexander,Reutskaya, Elena,Smirnov, Alexey,Korsakov, Mikhail,Krasavin, Mikhail
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Read Online
- Amidino substituted 2-aminophenols: biologically important building blocks for the amidino-functionalization of 2-substituted benzoxazoles
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Unlike the closely related and widely investigated amidino-substituted benzimidazoles and benzothiazoles with a range of demonstrated biological activities, the matching benzoxazole analogues still remain a largely understudied and not systematically evaluated class of compounds. To address this challenge, we utilized the Pinner reaction to convert isomeric cyano-substituted 2-aminophenols into their amidine derivatives, which were isolated as hydrochlorides and/or zwitterions, and whose structure was confirmed by single crystal X-ray diffraction. The key step during the Pinner synthesis of the crucial carboximidate intermediates was characterized through mechanistic DFT calculations, with the obtained kinetic and thermodynamic parameters indicating full agreement with the experimental observations. The obtained amidines were subjected to a condensation reaction with aryl carboxylic acids that allowed the synthesis of a new library of 5- and 6-amidino substituted 2-arylbenzoxazoles. Their antiproliferative features against four human tumour cell lines (SW620, HepG2, CFPAC-1, HeLa) revealed sub-micromolar activities on SW620 for several cyclic amidino 2-naphthyl benzoxazoles, thus demonstrating the usefulness of the proposed synthetic strategy and promoting amidino substituted 2-aminophenols as important building blocks towards biologically active systems.
- Pti?ek, Lucija,Hok, Lucija,Grb?i?, Petra,Topi?, Filip,Cetina, Mario,Rissanen, Kari,Paveli?, Sandra Kraljevi?,Vianello, Robert,Racané, Livio
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supporting information
p. 2784 - 2793
(2021/04/07)
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- Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses
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Today, there are no medicines to treat enterovirus and rhinovirus infections. In the present study, a series of novel pleconaril derivatives with substitutions in the isoxazole and phenyl rings was synthesized and evaluated for their antiviral activity against a panel of pleconaril-sensitive and -resistant enteroviruses. Studies of the structure-activity relationship demonstrate the crucial role of the N,N-dimethylcarbamoyl group in the isoxazole ring for antiviral activity against pleconaril-resistant viruses. In addition, one or two substituents in the phenyl ring directly impact on the spectrum of antienteroviral activity. The 3-(3-methyl-4-(3-(3-N,N-dimethylcarbamoyl-isoxazol-5-yl)propoxy)phenyl)-5-trifluoromethyl-1,2,4-oxadiazole 10g was among the compounds exhibiting the strongest activity against pleconaril-resistant as well as pleconaril-susceptible enteroviruses with IC50 values from 0.02 to 5.25 μM in this series. Compound 10g demonstrated markedly less CYP3A4 induction than pleconaril, was non-mutagenic, and was bioavailable after intragastric administration in mice. These results highlight compound 10g as a promising potential candidate as a broad spectrum enterovirus and rhinovirus inhibitor for further preclinical investigations.
- Egorova, Anna,Ekins, Sean,Jahn, Birgit,Kazakova, Elena,Makarov, Vadim,Schmidtke, Michaela
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- Tetrazole xanthine oxidase inhibitor compound as well as preparation method and application thereof
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The invention belongs to the technical field of medicines and relates to a tetrazole xanthine oxidase inhibitor compound as well as a preparation method and application thereof. The invention providesa tetrazole xanthine oxidase inhibitor compound shown as a general formula I or a pharmaceutically acceptable salt, an isomer, a polymorphic substance and a medicinal solvate and further provides anintermediate for preparing the tetrazole xanthine oxidase inhibitor compound or the pharmaceutically acceptable salt, and a structure of the intermediate is shown as a general formula II, III or IV, wherein R is described as claims and a description.
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Page/Page column 19
(2019/09/14)
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- Targeting the subpocket in xanthine oxidase: Design, synthesis, and biological evaluation of 2-[4-alkoxy-3-(1H-tetrazol-1-yl) phenyl]-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid derivatives
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Xanthine oxidase is an important target for the treatment of hyperuricemia, gout and other related diseases. Analysis of the high-resolution structure of xanthine oxidase with febuxostat identified the existence of a subpocket formed by the residues Leu648, Asn768, Lys771, Leu1014 and Pro1076. In this study, we designed and synthesized a series of 2-[4-alkoxy-3-(1H-tetrazol-1-yl) phenyl]-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid derivatives (8a-8z) with a tetrazole group targeting this subpocket of the xanthine oxidase active site, and they were further evaluated for their inhibitory potency against xanthine oxidase in vitro. The results showed that all the tested compounds (8a-8z) exhibited an apparent xanthine oxidase inhibitory potency, with IC50 values ranging from 0.0288 μM to 0.629 μM. Among them, compound 8u emerged as the most potent xanthine oxidase inhibitor, with an IC50 value of 0.0288 μM, which was comparable to febuxostat (IC50 = 0.0236 μM). The structure-activity relationship results revealed that the hydrophobic group at the 4′-position was indispensable for the inhibitory potency in vitro against xanthine oxidase. A Lineweaver-Burk plot revealed that the representative compound 8u acted as a mixed-type inhibitor for xanthine oxidase. Furthermore, molecular modeling studies were performed to gain insights into the binding mode of 8u with xanthine oxidase and suggested that the tetrazole group of the phenyl unit was accommodated in the subpocket, as expected. Moreover, a potassium oxonate-induced hyperuricemia model in rats was chosen to further confirm the hypouricemic effect of compound 8u, and the result demonstrated that compound 8u could effectively reduce serum uric acid levels at an oral dose of 5 mg/kg. In addition, acute oral toxicity study in mice indicated that compound 8u was nontoxic and tolerated at a dose up to 2000 mg/kg. Thus, compound 8u could be a potential and efficacious agent in treatment of hyperuricemia with low toxicity.
- Zhang, Bing,Dai,Bao, Ziyang,Mao, Qing,Duan,Yang,Wang, Shaojie
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- Iodine(III)-Catalyzed Electrophilic Nitration of Phenols via Non-Br?nsted Acidic NO2+ Generation
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The first catalytic procedure for the electrophilic nitration of phenols was developed using iodosylbenzene as an organocatalyst based on iodine(III) and aluminum nitrate as a nitro group source. This atom-economic protocol occurs under mild, non-Br?nsted acidic and open-flask reaction conditions with a broad functional-group tolerance including several heterocycles. Density functional theory (DFT) calculations at the (SMD:MeCN)Mo8-HX/(LANLo8+f,6-311+G) level indicated that the reaction proceeds through a cationic pathway that efficiently generates the NO2+ ion, which is the nitrating species under neutral conditions.
- Juárez-Ornelas, Kevin A.,Jiménez-Halla, J. Oscar C.,Kato, Terumasa,Solorio-Alvarado, César R.,Maruoka, Keiji
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supporting information
p. 1315 - 1319
(2019/03/07)
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- Compounds with xanthine oxidase inhibition activity, and preparation method and application thereof
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The invention belongs to the technical field of medicines, and relates to compounds with xanthine oxidase inhibition activity, and a preparation method and an application thereof. The invention provides the compounds with xanthine oxidase inhibition activity, represented by general formula I, or pharmaceutically acceptable salts, isomers, polymorphs and medical solvates thereof, and further provides an intermediate for preparing the compounds with xanthine oxidase inhibition activity, or the pharmaceutically acceptable salts thereof. The structure of the intermediate is represented by generalformula II or III shown in the description; and R in the general formulas is as defined in claims and the description.
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Paragraph 0072-0073
(2019/09/16)
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- ANTIBIOTIC COMPOUNDS
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The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.
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Page/Page column 77
(2018/03/25)
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- Improved schmidt conversion of aldehydes to nitriles using azidotrimethylsilane in 1,1,1,3,3,3-Hexafluoro-2-Propanol
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The Schmidt reaction of aromatic aldehydes using a substoichiometric amount (40 mol %) of triflic acid is described. Low catalyst loading was enabled by a strong hydrogen-bond-donating solvent hexafluoro-2-propanol (HFIP). This improved protocol tolerates a broad scope of aldehydes with diverse functional groups and the corresponding nitriles were obtained in good to high yields without the need for aqueous work up.
- Motiwala, Hashim F.,Yin, Qin,Aubé, Jeffrey
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- METHOD FOR PREPARING AFATINIB AND INTERMEDIATE THEREOF
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Revealed in the present invention is a method for preparing Afatinib (I): using 2-nitrile-4-[4-(N,N-dimethylamino)-I-oxo-2-buten-I-yl]amino-5-[(S)-(tetrahydrofuran-3-yl)oxy]aniline (II) and 4-fluoro-3-chloroaniline (III) as starting materials, and respectively performing a condensation and cyclization reaction with N,N-dimethylformamide dimethyl acetal (IV) to prepare Afatinib (I), wherein the method significantly reduces the manufacturing steps of Afatinib and greatly lower the costs. In addition, also provided in the present invention is a method for preparing an intermediate of Afatinib, wherein the method has a stable process, uses readily available starting materials, has a low cost, and all the reactions are classic reactions, suitable for meeting amplification requirements in the industry.
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Paragraph 0043; 0044
(2016/04/19)
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- A practical approach for regioselective mono-nitration of phenols under mild conditions
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Cu(NO3)2.3H2O was demonstrated to be an efficient, regioselective and inexpensive nitrating reagent for the synthesis of mono-nitro substituted phenolic compounds. 12 examples of different phenols were examined. Good yields (67-90%) have been achieved. ARKAT-USA, Inc.
- Chen, Ling-Yan,Liu, Tao,Zhou, Xiaokun,Sun, Zhihua
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- Microwave assisted synthesis of nitro phenols from the reaction of phenols with urea nitrate under acid-free conditions
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Urea nitrate was found to be an inexpensive, acid-free, and safe nitrating agent that provides mononitration of phenols and substituted phenols in excellent yields with exclusive ortho-selectivity under microwave irradiation. Microwave assisted reactions reduced the reaction times substantially and enhanced the product yields from good to excellent within shorter reaction times.
- Verma, Sanny,Pandita, Sangeeta,Jain, Suman L.
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p. 1320 - 1322
(2014/03/21)
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- Chemoselective Schmidt reaction mediated by triflic acid: Selective synthesis of nitriles from aldehydes
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An excellent utility of Schmidt reaction of aldehydes to access corresponding nitriles in an instantaneous reaction is demonstrated. The reaction of aldehydes with NaN3 and TfOH furnishes the corresponding nitriles in near quantitative yields and tolerates a variety of electron-withdrawing and electron-donating substituents on the substrates. Formanilides, a common side product in Schmidt reaction, is not observed in this reaction. Besides these advantages, the salient feature of this reaction is that it exhibits a remarkable chemoselectivity, as acid and ketone functionalities are well tolerated under the reaction conditions. The reaction is easily scalable, high yielding, and nearly instantaneous.
- Rokade, Balaji V.,Prabhu, Kandikere Ramaiah
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experimental part
p. 5364 - 5370
(2012/09/07)
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- Melamine-(H2SO4)3 and PVP-(H 2SO4)n as solid acids: Synthesis and application in the first mono- and di-nitration of bisphenol A and other phenols
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Melamine and poly vinylpyrrolidone (PVP) reacted with neat sulfuric acid readily to form two new organic solid acids namely melamine-(H 2SO4)3 and PVP-(H2SO 4)n. These solid acids were used for the first nitration of bisphenol A as well as other phenols in the presence of NH4NO 3. Mono- and di-nitro bisphenol A have been characterized with IR and 1H NMR techniques.
- Chehardoli, Gholamabbas,Zolfigol, Mohammad Ali,Azimi, Seyedeh Bahareh,Alizadeh, Ebadollah
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experimental part
p. 827 - 830
(2012/02/14)
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- Non-steroidal dissociated glucocorticoid agonists: Indoles as A-ring mimetics and function-regulating pharmacophores
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We report a SAR of non-steroidal glucocorticoid mimetics that utilize indoles as A-ring mimetics. Detailed SAR is discussed with a focus on improving PR and MR selectivity, GR agonism, and in vitro dissociation profile. SAR analysis led to compound (R)-33 which showed high PR and MR selectivity, potent agonist activity, and reduced transactivation activity in the MMTV and aromatase assays. The compound is equipotent to prednisolone in the LPS-TNF model of inflammation. In mouse CIA, at 30 mg/kg compound (R)-33 inhibited disease progression with an efficacy similar to the 3 mg/kg dose of prednisolone.
- Betageri, Raj,Gilmore, Thomas,Kuzmich, Daniel,Kirrane, Thomas M.,Bentzien, J?rg,Wiedenmayer, Dieter,Bekkali, Younes,Regan, John,Berry, Angela,Latli, Bachir,Kukulka, Alison J.,Fadra, Tazmeen N.,Nelson, Richard M.,Goldrick, Susan,Zuvela-Jelaska, Ljiljana,Souza, Don,Pelletier, Josephine,Dinallo, Roger,Panzenbeck, Mark,Torcellini, Carol,Lee, Heewon,Pack, Edward,Harcken, Christian,Nabozny, Gerald,Thomson, David S.
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scheme or table
p. 6842 - 6851
(2011/12/22)
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- Bromodimethylsulfonium bromide/tetrabutylammonium nitrite: An efficient catalyst mixture for the nitration of phenols
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Nitrophenols were obtained via direct nitration of phenols with tetrabutylammonium nitrite in the presence of bromodimethylsulfonium bromide at room temperature in high yields under aprotic conditions. TUeBITAK.
- Akhlaghinia, Batool,Pourali, Alireza
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experimental part
p. 753 - 759
(2010/12/18)
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- PEG-N2O4: An efficient nitrating agent for the selective mono- and dinitration of phenols under mild conditions
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N2O4 was easily impregnated on polyethyleneglycol to give a stable reagent. The polyethyleneglycol-N2O4 (PEG-N2O4) system was used as an effective nitrating agent for the nitration of phenols. Mono- and dinitrophenols can be obtained via direct nitration of phenols in the presence of PEG-N2O4 at room temperature in moderate to high yields. Copyright Taylor & Francis Group, LLC.
- Zolfigol, Mohammad Ali,Madrakian, Elaheh,Ghaemi, Ezat,Niknam, Khodabakhsh
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p. 3366 - 3374
(2008/12/22)
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- Palladium-catalyzed C-O bond formation: direct synthesis of phenols and aryl/alkyl ethers from activated aryl halides
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A simple and efficient palladium-catalyzed carbon-oxygen bond formation is reported. The palladium-tri-tert-butylphosphine complex was found to be effective in converting haloarenes to corresponding substituted phenols. This methodology offers a direct transformation of aryl halides to phenols, as well as the straightforward application to generate a wide variety of diaryl or alkyl/aryl ethers.
- Chen, Guoshu,Chan, Albert S.C.,Kwong, Fuk Yee
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p. 473 - 476
(2008/02/03)
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- Tribromoisocyanuric acid/NaNO2: A new reagent for mononitration of phenols under mild and heterogeneous conditions
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Nitrophenols can be obtained via direct nitration of phenols with tribromoisocyanuric acid, NaNO2 and wet SiO2 at room temperature in good to high yields.
- Niknam, Khodabakhsh,Zolfigol, Mohammad Ali,Madrakian, Elaheh,Ghaemi, Ezat
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p. 109 - 112
(2008/09/17)
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- BENZOTHIAZOLES HAVING HISTAMINE H3 RECEPTOR ACTIVITY
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Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (l): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.
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Page/Page column 60-61
(2008/06/13)
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- 1,3-Dihalo-5,5-dimethylhydantoin or citric acid/NaNO2 as a heterogeneous system for the selective mononitration of phenols under mild conditions
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Direct nitration of phenols was performed using 1,3-dichloro-5,5- dimethylhydantoin, 1,3-dibromo-5,5-dimethylhydantoin or citric acid/NaNO 2 in the presence of wet SiO2 at room temperature.
- Zolfigol, Mohammad A.,Ghaemi, Ezat,Madrakian, Elaheh,Choghamarani, Arash G.
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- Silica chloride/NaNO2 as a novel heterogeneous system for the nitration of phenols under mild conditions
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Nitrophenols can be obtained via direct nitration of phenols with silica chloride, NANO2, and wet SiO2 at room temperature in moderate to high yields.
- Zolfigol, Mohammad Ali,Shirini, Farhad,Chogamarani, Arash Ghorbani
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p. 2019 - 2025
(2007/10/03)
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- Trichloroisocyanuric acid/NaNO2 as a novel heterogeneous system for the selective mononitration of phenols under mild conditions
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Nitrophenols can be obtained via direct nitration of phenols with trichloroisocyanuric acid, NaNO2 and wet SiO2 at room temperature in moderate to high yields.
- Zolfigol, Mohammad Ali,Ghaemi, Ezat,Madrakian, Elaheh
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p. 191 - 194
(2007/10/03)
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- Silica sulfuric acid/NaNO2 as a novel heterogeneous system for the nitration of phenols under mild conditions
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Nitrophenols can be obtained in moderate to high yields via nitrosation-oxidation of phenols with silica sulfuric acid, NaNO2 and wet SiO2 at room temperature. In situ generation of HNO2 and a radical cation mechanism via the nitrous acid catalyzed (NAC) pathway appear to be applicable to phenol nitration using these reagents.
- Zolfigol, Mohammad Ali,Madrakian, Elahe,Ghaemi, Ezat
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p. 734 - 742
(2007/10/03)
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- Nitration of phenols under mild and heterogeneous conditions
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Nitrophenols can be obtained in moderate to high yields using a combination of Mg(HSO4)2 or NaHSO4.H2O, NaNO3 and wet SiO2 in dichloromethane at room temperature.
- Zolfigol, Mohammad Ali,Ghaemi, Ezat,Madrakian, Elahe
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p. 614 - 620
(2007/10/03)
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- An efficient method for chemoselective nitration of phenols under mild and heterogeneous conditions
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Nitrophenols can be obtained via nitrosation-oxidation of phenols with Mg(HSO4)2 or NaHSO4.H2O, NaNO2 and wet SiO2 at room temperature in moderate to high yields. In situ generation of HNO2 and radical cation mechanism via nitrous acid catalyzed (NAC) pathway appear to be applicable to phenol nitration using these reagents.
- Zolfigol,Madrakian,Ghaemi
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p. 1191 - 1195
(2007/10/03)
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- One-pot nitration of phenols under mild and heterogeneous conditions
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Nitrophenols can be obtained via nitrosation-oxidation of phenols with Oxone, NaNO2 and wet SiO2 at room temperature in moderate to high yields. In situ generation of HNO2 and the radical cation mechanism via the nitrous acid catalysed (NAC) pathway or hydrogen abstraction involving NO2 appear to be applicable to phenol nitration using these reagents.
- Zolfigol,Bagherzadeh,Madrakian,Ghaemi,Taqian-Nasab
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p. 140 - 142
(2007/10/03)
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- Unexpected side products in the tetramethylammonium fluoride-dimethylsulphoxide system
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Reactions of chloro- and nitro-aromatics with low water content solutions of TMAF in DMSO can lead to complex product mixtures resulting from activation of DMSO by fluoride and the formation of DMSO-derived products. Also, the system has been shown to give hydrolysis products in addition to the well-known ethers and phenols, with carboxylic acids and benzamides being formed from the attempted fluorodenitration of substituted benzonitriles.
- Adams, Dave J.,Clark, James H.,McFarland, Heather,Nightingale, David J.
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- The effect of basicity on fluorodenitration reactions using tetramethylammonium salts
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The fluorodenitration of several nitroaromatics with tetramethylammonium salts has been found to be dependent on the basicity of the fluorinating species. Tetramethylammonium fluoride is highly basic and is capable of inducing H-D exchange in 1,3-dinitrobenzene, as well as deprotonating N,N- dimethylacetamide. Reaction of the fluoride with phthalic anhydride forms the bifluoride in situ. Tetramethylammonium bifluoride gives higher yields of the required fluoroaromatic, but slower reaction rates than the corresponding fluoride.
- Adams, Dave J.,Clark, James H.,Nightingale, David J.
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p. 7725 - 7738
(2007/10/03)
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- Nitration and hydroxylation of substituted phenols by peroxynitrite. Kinetic feature and an alternative mechanistic view
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The reaction of peroxynitrite (ONOO-) with a series of para-substituted phenols has been examined in aqueous phosphate buffer and acetonitrile solutions. Major products were the corresponding 2-nitro derivative and the 4-substituted catechol. Kinetic study showed good correlation with Hammett σ(p)+ parameters and reduction potentials, suggesting the possible one-electron transfer process involving the nitrosoniun ion (NO+) as initial electrophile generated from peroxynitrous acid.
- Nonoyama, Nobuaki,Chiba, Kazuhiko,Hisatome, Kaori,Suzuki, Hitomi,Shintani, Futoshi
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p. 6933 - 6937
(2007/10/03)
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- 2-arylthiazole derivatives and pharmaceutical composition thereof
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Pharmaceutical compositions for treating gout or hyperuricemia and containing a new categorized compound, i.e. 2-arylthiazole derivatives, as an active ingredient, are provided. The 2-arylthiazole derivatives in the present invention are represented by the following formula (I): STR1 wherein Ar is an unsubstituted or substituted pyridyl, thienyl, furyl, naphthyl or phenyl group; X is a hydrogen atom, alkyl group or carboxyl group which may be protected, and Y is a hydrogen atom, alkyl group, or a hydroxyl or carbonyl group which may be protected. Furthermore, novel compounds included in the 2-arylthiazole derivatives and pharmaceutically acceptable salts thereof are provided.
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- Facile rearrangements of alkynylamino heterocycles with noble metal cations
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A number of 2-(alkynylamino)-substituted heterocycles have been synthesized. These heterocycles rearrange in the presence of silver(I) and gold(I) salts to give novel 2H-pyrimido[2,1-b]benzoxazoles, 2H-pyrimido[2,1-b]benzothiazoles, and a 2H-pyrimido[2,1-b]benzoselenazole. Two of the the 2H-pyrimido[2,1-b]benzoxazoles were isolated in good yield. The kinetics of the silver tetrafluoroborate-catalyzed rearrangements of selected (alkynylamino)benzoxazoles and benzothiazoles have been examined by 1H NMR in CD3CN. Factors affecting the electron densities of the triple bond and of the nitrogen atom in the heterocycle are important in influencing the rate of rearrangement.
- Lok, Roger,Leone, Ronald E.,Williams, Antony J.
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p. 3289 - 3297
(2007/10/03)
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- MONONITRATION DE PHENOLS PAR DES NITRATES METALLIQUES
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A new and practical route to mononitrphenol in high yields is described using commercially aviable hydrated metallic nitrates.According to the metallic nitrate used, this reaction can yield regiospecifically the ortho-nitrophenol or regioselectively the para-nitrophenol.This method is successfully applied to some phenolic derivatives, in particular to the preparation of 2-nitroestrone.Sodium nitrate with ferric chloride or with titane tetrachloride allows mononitration of phenol.
- Poirier, Jean-Marie,Vottero, Catherine
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p. 1415 - 1422
(2007/10/02)
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- NITRATION OF PHENOLS BY CLAY-SUPPORTED FERRIC NITRATE
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"Clayfen", a reactive form of ferric nitrate stabilized by adsorption unto an acidic K 10 clay, is an efficient and selective nitrating agent of phenols, under very mild conditions.It leads specifically to mononitration, with high regioselectivities.These characteristics, coupled with its low cost, ease of preparation and the simplicity of experimental procedures, make "clayfen" an attractive nitrating reagent.
- Cornelis, A.,Laszlo, P.,Pennetreau, P.
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p. 961 - 972
(2007/10/02)
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