- Proton type ionic liquid [HDBN] [2-PyOH] and preparation and application thereof
-
The invention discloses proton type ionic liquid [HDBN] [2-PyOH] and preparation and application thereof, and belongs to the technical field of catalysts. The preparation method comprises the steps that 1, 5-diazabicyclo [4.3. 0] nonyl-5-ene reacts with 2-hydroxypyridine to prepare protonic ionic liquid [HDBN] [2-PyOH]; and as a catalyst, the ionic liquid can catalyze CO2 and o-aminobenzonitrile compounds to efficiently react under mild conditions to obtain a series of quinazoline-2, 4 (1H, 3H)-diketone compounds. The proton type ionic liquid catalyst has the advantages of simple synthesis process, excellent catalytic performance, good substrate expansion capability, easy product separation and the like, and has a good industrial application prospect.
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-
Paragraph 0021; 0025-0029; 0060-0064
(2021/11/21)
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- Method for preparing 2,4-(1H,3H)-quinazoline diketone compound
-
The invention discloses a method for preparing a 2,4-(1H,3H)-quinazoline diketone compound. A 2-aminobenzonitrile compound as shown in a formula (1) and carbon dioxide are used as raw materials and react in 2-hydroxypyridine ionic liquid to obtain the 2,4-(1H,3H)-quinazoline diketone compound as shown in a formula (II), and the reaction formula is as shown in the specification. When the ionic liquid is applied to the reaction for preparing the 2,4-(1H,3H)-quinazoline diketone compound, the reaction condition is mild, the separation and purification process of the product is simple, the product yield is high, and the substrate application range is wide.
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-
Paragraph 0055-0057; 0065
(2021/05/12)
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- Synthesis of acyclic nucleoside phosphonates targeting flavin-dependent thymidylate synthase in Mycobacterium tuberculosis
-
Flavin-Dependent Thymidylate Synthase (FDTS) encoded by ThyX gene was discovered as a new class of thymidylate synthase involved in the de novo synthesis of dTMP named only in 30 % of human pathogenic bacteria. This target was pursed for the development of new antibacterial agents against multiresistant pathogens. We have developed a new class of ANPs based on the mimic of two natural's cofactors (dUMP and FAD) as inhibitors against Mycobacterium tuberculosis ThyX. Several synthetic efforts were performed to optimize regioselective N1-alkylation, cross-coupling metathesis and Sonogashira cross-coupling. Compound 19c showed a poor 31.8% inhibitory effect on ThyX at 200 μM.
- Agrofoglio, Luigi A.,Becker, Hubert F.,Biteau, Nicolas G.,Lambry, Jean-Christophe,Myllykallio, Hannu,Roy, Vincent
-
-
- N2N N4-disubstituted quinazoline-2,4-diamines and uses thereof
-
Described herein are quinazoline-based compounds and formulations thereof. In some embodiments, the compounds and/or formulations thereof can be effective to inhibit and/or kill A. baumannii. Also described herein are methods of treating a subject in need thereof by administering to the subject in need thereof a quinazoline-based compound and/or formulation thereof to the subject in need thereof.
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Page/Page column 46-47; 49
(2019/07/03)
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- Efficient synthesis of 2-oxazolidinones and quinazoline-2,4(1H,3H)-diones from CO2 catalyzed by tetrabutylammonium fluoride
-
By employing tetrabutylammonium fluoride (TBAF) as a catalyst, the various carboxylative cyclizations of the propargylic amines having internal alkynes with CO2 proceeded to afford the corresponding 2-oxazolidinones. In this case, it was also found that the generated 2-oxazolidinones were tautomerized into the corresponding 2-oxazolones due to the basicity of TBAF. In addition, we performed the synthesis of quinazoline-2,4(1H,3H)-dione from 2-aminobenzonitrile and CO2 by using TBAF as a catalyst.
- Fujii, Akira,Matsuo, Hideaki,Choi, Jun-Chul,Fujitani, Tadahiro,Fujita, Ken-ichi
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p. 2914 - 2920
(2018/05/16)
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- CO2 transformation under mild conditions using tripolyphosphate-grafted KCC-1-NH2
-
Fibrous nanosilica (KCC-1) as a catalyst support was investigated in terms of stability, recycling, and reusability. For the first time, CO2 transformation was performed via the synthesis and application of KCC-1 together with sodium tripolyphosphate (STPP) and 3-aminopropyltriethoxysilane (APTES) as its functionalized derivative. To this goal, KCC-1/STPP NPs were applied to act as a nanocatalyst with excellent catalytic activities under green reaction conditions.
- Sadeghzadeh, Seyed Mohsen,Zhiani, Rahele,Moradi, Marjan
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p. 535 - 544
(2018/04/26)
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- Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation
-
The heterocyclizations from various methyl (2-nitrobenzoyl)carbamates to substituted quinazoline-2,4(1H,3H)-diones under hydrogenation conditions were investigated in this study. In the presence of p-toluenesulfonic acid monohydrate in methanol, various q
- Wang, Peng-Xu,Wang, Ya-Nan,Lin, Zi-Yun,Li, Gang,Huang, Hai-Hong
-
supporting information
p. 1183 - 1189
(2018/04/02)
-
- A 2, 4 - quinazoline dione compound preparation method
-
The invention belongs to the field of organic chemistry, and concretely relates to a preparation method of benzoyleneurea compounds. The preparation method comprises the following steps: a 2-aminobenzonitrile compound and carbon dioxide are used as raw materials, preferably a reaction employs acylamino divalent rare earth metal amides and DBU as catalysts at 50-150 DEG C under a normal pressure, the reaction is carried out in an aprotic polar solvent for 4-40 hours, and the benzoyleneurea compounds are obtained with a high yield. The method has the advantages of mild reaction condition, few catalyst amount, simple separation and purification, high yield and wide substrate application range.
- -
-
Paragraph 0118; 0119
(2017/10/31)
-
- AMINOISOXAZOLINE COMPOUNDS AS AGONISTS OF ALPHA7-NICOTINIC ACETYLCHOLINE RECEPTORS
-
The present invention relates to novel aminoisoxazoline compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
- -
-
Paragraph 00422; 00423
(2017/05/19)
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- Characterizing the antimicrobial activity of N2,N4-disubstituted quinazoline-2,4-diamines toward multidrug-resistant Acinetobacter baumannii
-
We previously reported a series of N2,N4-disubstituted quinazoline-2,4- diamines as dihydrofolate reductase inhibitors with potent in vitro and in vivo antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) strains. In this work, we extended our previous study to the Gram-negative pathogen Acinetobacter baumannii. We determined that optimized N2,N4-disubstituted quinazoline-2,4-diamines are strongly antibacterial against multidrug-resistant A. baumannii strains when the 6-position is replaced with a halide or an alkyl substituent. Such agents display potent antibacterial activity, with MICs as low as 0.5 μM, while proving to be strongly bactericidal. Interestingly, these compounds also possess the potential for antibiofilm activity, eradicating 90% of cells within a biofilm at or near MICs. Using serial passage assays, we observed a limited capacity for the development of resistance toward these molecules (4-fold increase in MIC) compared to existing folic acid synthesis inhibitors, such as trimethoprim (64-fold increase) and sulfamethoxazole (128-fold increase). We also identified limited toxicity toward human cells, with 50% lethal doses (LD50s) of ≤23 μM for lead agents 4 and 5. Finally, we demonstrated that our lead agents have excellent in vivo efficacy, with lead agent 5 proving more efficacious than tigecycline in a murine model of A. baumannii infection (90% survival versus 66%), despite being used at a lower dose (2 versus 30 mg kg-1). Together, our results demonstrate that N2,N4-disubstituted quinazoline-2,4-diamines have strong antimicrobial and antibiofilm activities against both Gram-positive organisms and Gram-negative pathogens, suggesting strong potential for their development as antibacterial agents.
- Fleeman, Renee,Van Horn, Kurt S.,Barber, Megan M.,Burda, Whittney N.,Flanigan, David L.,Manetsch, Roman,Shaw, Lindsey N.
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supporting information
(2017/05/31)
-
- Synthesis and Characterization of Amidato Divalent Lanthanide Complexes and Their Use in Forming 2,4-Quinazolidinones from CO2 and 2-Aminobenzonitriles
-
Four amidato divalent lanthanide complexes, {LnLn[N(TMS)2]THF}2 [n = 1, Ln = Eu (1); n = 2, Ln = Eu (3), Yb (4); HL1 = tBuC6H4CONHC6H3(iPr)2; HL2 = C6H5CONHC6H3(iPr)2] and {L3Eu[N(TMS)2]THF}{L32Eu(THF)2} (2) [HL3 = ClC6H4CONHC6H3(iPr)2], were synthesized and extensively characterized. This is the first time that the amidato lanthanide amides 1-4 were used to catalyze the reactions of CO2 and 2-aminobenzonitriles to form quinazoline-2,4(1H,3H)-diones at atmospheric pressure. All the complexes efficiently catalyzed the transformation, with complex 3 showing the highest activity. This catalytic system gave good to excellent yields, and good functional group tolerance. Preliminary studies were conducted to investigate the reaction mechanism.
- Wang, Qianyu,Lu, Chengrong,Zhao, Bei,Yao, Yingming
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p. 2555 - 2559
(2016/06/01)
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- Spidery catalyst for the synthesis of quinazoline-2,4(1H,3H)-diones
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In this study, a novel fibrous nanosilica (KCC-1) based nanocatalyst (Au, Pd, and Cu) with a high surface area and easy accessibility of active sites was successfully developed by a facile approach. KCC-1 with a high surface area was functionalized with multi-carboxylic hyperbranched polyglycerol groups (HPG) acting as robust anchors so that the metal nanoparticles (Au, Pd, and Cu) were well-dispersed on the fibers of the KCC-1 microspheres without aggregation. Because of the amplification effect of HPG, high loading capacities of the nanocatalysts were achieved. The synthesized KCC-1/HPG/X nanocatalyst exhibited excellent catalytic activity for the synthesis of quinazoline-2,4(1H,3H)-diones from CO2 and 2-aminobenzonitrile under mild conditions due to the easy accessibility of the active sites. High catalytic activity and ease of recovery from the reaction mixture by using filtration after several reuses without any significant loss of performance are additional eco-friendly attributes of this catalytic system.
- Sadeghzadeh, Seyed Mohsen
-
p. 1435 - 1441
(2016/03/09)
-
- Octahydropyrrole[3, 4-c]pyrrole derivative and using method and application thereof
-
The invention relates to an ctahydropyrrole[3, 4-c]pyrrole derivative and a using method and application thereof. A compound and a drug composition containing the same are used for resisting orexin receptors. The invention further relates to methods of pr
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-
Paragraph 0182; 0281; 0283; 0284
(2018/02/04)
-
- Amino-functionalized carbon nanofibres as an efficient metal free catalyst for the synthesis of quinazoline-2,4(1H,3H)-diones from CO2 and 2-aminobenzonitriles
-
Carbon nanofibres (CNFs) functionalized with 4-amino-2,6-dimethylpyridine were found to be an efficient metal free catalyst for the synthesis of quinazoline-2,4(1H,3H)-diones from CO2 and 2-aminobenzonitriles using water as a reaction medium. The presence of water they exhibited a remarkable enhancement in reaction rates and provided high to excellent yield of the products. After completion of the reaction, the catalyst was easily separated by centrifugation and was successfully reused for several runs without showing any significant decrease in catalytic activity.
- Kumar, Subodh,Verma, Sanny,Shawat, Efrat,Nessim, Gilbert Daniel,Jain, Suman L.
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p. 24670 - 24674
(2015/03/30)
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- Ionic liquid immobilized onto fibrous nano-silica: A highly active and reusable catalyst for the synthesis of quinazoline-2,4(1 H,3 H)-diones
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In this study, a novel fibrous nano-silica (KCC-1) supported ionic liquid (KCC-1/IL) with high surface area and easy accessibility of active sites was successfully developed by a facile approach. The synthesized KCC-1/IL nanocatalyst exhibited excellent catalytic activity for the synthesis of quinazoline-2,4(1 H,3 H)-diones from CO2 and 2-aminobenzonitriles under mild conditions to the easy accessibility of the active sites. A high catalytic activity and ease of recovery from the reaction mixture by using filtration and several reuses without any significant loss in performance are additional eco-friendly attributes of this catalytic system.
- Sadeghzadeh, Seyed Mohsen
-
-
- Synthesis and antimicrobial activity of amino linked heterocycles
-
Amino-linked benzoxazolyl/benzothiazolyl/benzimidazolyl quinazolines were prepared and their antimicrobial activity studied. The nitro-substituted benzothiazolyl quinazoline (8f) may be a potential antibacterial agent against Staphylococcus aureus and nitro-substituted benzimidazolyl quinazoline (9f) may be a potential antifungal agent against Aspergillus niger.
- Mallikarjuna Reddy, Lingaladinne,Dinneswara Reddy, Guda,Padmaja, Adivireddy,Padmavathi, Venkatapuram
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-
- Synthesis and evaluation of quinazolines as inhibitors of the bacterial cell division protein FtsZ
-
The bacterial cell division protein FtsZ is one of many potential targets for the development of novel antibiotics. Recently, zantrin Z3 was shown to be a cross-species inhibitor of FtsZ; however, its specific interactions with the protein are still unknown. Herein we report the synthesis of analogues that contain a more tractable core structure and an analogue with single-digit micromolar inhibition of FtsZs GTPase activity, which represents the most potent inhibitor of Escherichia coli FtsZ reported to date. In addition, the zantrin Z3 core has been converted to two potential photo-cross-linking reagents for proteomic studies that could shed light on the molecular interactions between FtsZ and molecules related to zantrin Z3.
- Nepomuceno, Gabriella M.,Chan, Katie M.,Huynh, Valerie,Martin, Kevin S.,Moore, Jared T.,Obrien, Terrence E.,Pollo, Luiz A. E.,Sarabia, Francisco J.,Tadeus, Clarissa,Yao, Zi,Anderson, David E.,Ames, James B.,Shaw, Jared T.
-
p. 308 - 312
(2015/03/30)
-
- Amine functionalized MCM-41: An efficient heterogeneous recyclable catalyst for the synthesis of quinazoline-2,4(1H,3H)-diones from carbon dioxide and 2-aminobenzonitriles in water
-
A simple covalently linked amine functionalized MCM-41 compound was investigated using mesoporous catalytic protocols as a highly efficient, heterogeneous and recyclable catalyst for the synthesis of a wide variety of quinazoline-2,4(1H,3H)-dione derivatives from 2-aminobenzonitriles and carbon dioxide in aqueous reaction medium. This catalytic system represents a heterogeneous and environmentally benign protocol. The effect of various reaction parameters, such as the influences of solvent, temperature, CO 2 pressure, and time for the synthesis of quinazoline-2,4(1H,3H)- diones were studied. The developed protocol can be applied for the synthesis of the most important key intermediate 6,7-dimethoxyquinazoline-2,4(1H,3H)-dione and several biologically active derivatives such as Prazosin, Bunazosin and Doxazosin. Besides this, the developed catalyst could be reused for five consecutive recycles without any significant loss in its catalytic activity. The amine functionalized MCM-41 catalyst was characterized by various characterization techniques such as FT-IR, TGA/DTA, XRD, Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), and solid state 29Si CP MAS NMR analysis. This journal is the Partner Organisations 2014.
- Nale, Deepak B.,Rana, Surjyakanta,Parida, Kulamani,Bhanage, Bhalchandra M.
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p. 1608 - 1614
(2014/06/09)
-
- Antileishmanial activity of a series of N2, N 4-disubstituted quinazoline-2,4-diamines
-
A series of N2,N4-disubstituted quinazoline-2,4- diamines has been synthesized and tested against Leishmania donovani and L. amazonensis intracellular amastigotes. A structure-activity and structure-property relationship study was conducted in part using the Topliss operational scheme to identify new lead compounds. This study led to the identification of quinazolines with EC50 values in the single digit micromolar or high nanomolar range in addition to favorable physicochemical properties. Quinazoline 23 also displayed efficacy in a murine model of visceral leishmaniasis, reducing liver parasitemia by 37% when given by the intraperitoneal route at 15 mg kg-1 day-1 for 5 consecutive days. Their antileishmanial efficacy, ease of synthesis, and favorable physicochemical properties make the N2,N 4-disubstituted quinazoline-2,4-diamine compound series a suitable platform for future development of antileishmanial agents.
- Van Horn, Kurt S.,Zhu, Xiaohua,Pandharkar, Trupti,Yang, Sihyung,Vesely, Brian,Vanaerschot, Manu,Dujardin, Jean-Claude,Rijal, Suman,Kyle, Dennis E.,Wang, Michael Zhuo,Werbovetz, Karl A.,Manetsch, Roman
-
p. 5141 - 5156
(2014/07/08)
-
- Efficient [WO4]2--catalyzed chemical fixation of carbon dioxide with 2-aminobenzonitriles to quinazoline-2,4(1 H,3 H)-diones
-
A simple monomeric tungstate, TBA2[WO4] (I, TBA = tetra-n-butylammonium), could act as an efficient homogeneous catalyst for chemical fixation of CO2 with 2-aminobenzonitriles to quinazoline-2,4(1H,3H)-diones. Various kinds of structurally diverse 2-aminobenzonitriles could be converted into the corresponding quinazoline-2,4(1H,3H)-diones in high yields at atmospheric pressure of CO 2. Reactions of inactive 2-amino-4-chlorobenzonitrile and 2-amino-5-nitrobenzonitrile at 2 MPa of CO2 also selectively proceeded. The present system was applicable to a g-scale reaction of 2-amino-5-fluorobenzonitrile (10 mmol scale) with CO2 and 1.69 g of analytically pure quinazoline-2,4(1H,3H)-dione could be isolated. In this case, the turnover number reached up to 938 and the value was the highest among those reported for base-mediated systems so far. NMR spectroscopies showed formation of the corresponding carbamic acid through the simultaneous activation of both 2-aminobenzonitirile and CO2 by I. Kinetic and computational studies revealed that I plays an important role in conversion of the carbamic acid into the product.
- Kimura, Toshihiro,Sunaba, Hanako,Kamata, Keigo,Mizuno, Noritaka
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p. 13001 - 13008
(2013/02/22)
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- Design, synthesis, and biological evaluation of new diaminoquinazolines as β-catenin/Tcf4 pathway inhibitors
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More than 50 new diaminoquinazoline derivatives have been synthesized and evaluated in a colon carcinoma cell growth inhibition assay using HCT116 and SW480 cells. Twenty compounds with good cell growth inhibitory activities (50 values 50 values of 1.5-2.5 μM for HCT116 cells with the luciferase reporter assay.
- Mao, Yongjun,Lin, Nan,Tian, Wang,Han, Xiaofeng,Han, Xiaobing,Huang, Ziwei,An, Jing
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experimental part
p. 1346 - 1359
(2012/04/04)
-
- Ligand based design of novel histamine H4 receptor antagonists; Fragment optimization and analysis of binding kinetics
-
The histamine H4 receptor is a G protein-coupled receptor that has attracted much interest for its role in inflammatory and immunomodulatory functions. In our search for new H4R ligands, a low affinity isoquinoline fragment was optimized to 7-(furan-2-yl)-4-(piperazin-1-yl) quinazolin-2-amine (VUF11489), as a new H4R antagonist. Analysis of its binding kinetics at the human H4R showed this compound to have a very different dissociative half-life in comparison with reference antagonist JNJ7777120.
- Smits, Rogier A.,Lim, Herman D.,Van Der Meer, Tiffany,Kuhne, Sebastiaan,Bessembinder, Karin,Zuiderveld, Obbe P.,Wijtmans, Maikel,De Esch, Iwan J.P.,Leurs, Rob
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supporting information; experimental part
p. 461 - 467
(2012/02/04)
-
- Alkali metal cations control over nucleophilic substitutions on aromatic fused pyrimidine-2,4-[1H,3H]-diones: Towards new PNA monomers
-
In this paper we report synthesis of a series of aromatic fused pyrimidine-2,4(3H)-dione-1-yl acetic acid and new PNA monomers containing these polycyclic nucleobase analogues. Introduction of a fused aromatic ring onto the 5,6-positions of the pyrimidine-2,4-[1H,3H]-diones brings about the steric effects and the charge delocalization, both weakening the nucleophilic substitutions on the 1- and 3-positions. We found that alkali metal cations play an important role in this alkylation reaction. LiOH brings out a much more efficient alkylation than NaOH does, while KOH nearly does not work on this reaction. Such influences from the alkali metal cations are probably due to that the charge-pairing interactions between the pyrimidine-2,4-dioxide anions and the alkali metal cations rearrange the charge distribution around the whole aromatic system and increase the negative charge distribution on the 1- and 3-nitrogen atoms, which then strengthens the nucleophilic reactivity on these positions.
- Li, Pengfa,Zhan, Chuanlang,Zhang, Shanlin,Ding, Xunlei,Guo, Fengqi,He, Shenggui,Yao, Jiannian
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p. 8908 - 8915
(2012/10/29)
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- PHARMACEUTICAL COMPOUNDS AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF
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Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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Page/Page column 17-18
(2010/04/23)
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- A new and facile synthesis of quinazoline-2,4(1 H,3H)-diones
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A new and facile preparation of quinazoline-2,4(1H,3H)-diones was first reported which was the condensation of aromatic o-aminonitriles with DMF or N,N-diethylformamide in the presence of ZnCl2 (0.5-10 mol %) at 190-200 °C in the sealed reactor
- Jiarong, Li,Xian, Chen,Daxin, Shi,Shuling, Ma,Qing, Li,Qi, Zhang,Jianhong, Tang
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supporting information; body text
p. 1193 - 1196
(2009/08/07)
-
- Discovery and structure-activity relationships of 4-aminoquinazoline derivatives, a novel class of opioid receptor like-1 (ORL1) antagonists
-
Synthesis and structure-activity relationship studies of a series of 4-aminoquinazoline derivatives led to the identification of (1R,2S)-17, N-[(1R,2S)-2-({2-[(4-chlorophenyl)carbonyl]amino-6-methylquinazolin-4-yl}amino)cyclohexyl]guanidine dihydrochloride, as a highly potent ORL1 antagonist with up to 3000-fold selectivity over the μ, δ, and κ opioid receptors. Molecular modeling clarified the structural factors contributing to the high affinity and selectivity of (1R,2S)-17.
- Okano, Masahiko,Mito, Jun,Maruyama, Yasufumi,Masuda, Hirofumi,Niwa, Tomoko,Nakagawa, Shin-ichiro,Nakamura, Yoshitaka,Matsuura, Akira
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experimental part
p. 119 - 132
(2011/02/25)
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- Azido-Schmidt reaction for the formation of amides, imides and lactams from ketones in the presence of FeCl3
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Ketones undergo smooth rearrangement with TMSN3 in the presence of FeCl3 under extremely mild conditions to provide the corresponding amides, imides and lactams in good yields with high selectivity. This method is very useful for the preparation of a wide range of amides, imides and lactams from ketones. The use of FeCl3 makes this method simple, convenient and cost-effective.
- Yadav,Reddy, B.V. Subba,Reddy, U.V. Subba,Praneeth
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p. 4742 - 4745
(2008/12/21)
-
- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
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Page/Page column 49
(2010/11/30)
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- Synthesis of new quinazoline-2,4(1H,3H)-dione non-nucleoside analogues of the reverse transcriptase inhibitor TNK-651
-
The synthesis is described of a series of new non-nucleoside analogues of the reverse transcriptase inhibitor TNK-651 from quinazoline-2,4(1H,3H)-diones. Compounds 2a-c were silylated and treated with benzyl chloromethyl ether in the presence of CsI to give 1-benzyloxymethylquinazoline derivatives 3a-c. Treatment of the silylated quinazolinediones 2a-c with the appropriate acetals 5a-e in the presence of TMS triflate afforded the corresponding TNK-651 analogues 6-10.
- El-Brollosy, Nasser R.
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p. 358 - 361
(2008/02/11)
-
- METHOD OF TREATING BRAIN CANCER
-
Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.
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Page/Page column 49
(2008/06/13)
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- COMPOUNDS AND THERAPEUTICAL USE THEREOF
-
Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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- PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSYNE KINASES
-
Compounds of formula (I): and their use in the inhibition of Trk activity are described.
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Page/Page column 110
(2008/06/13)
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- NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
-
A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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- NOVEL QUINAZOLINE DERIVATIVES AND METHODS OF TREATMENT RELATED TO THE USE THEREOF
-
The present invention relates to novel compounds of Formula (I): which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.
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-
- A Simple One-Step Synthesis of 3-Amino-2,4(1H,3H)quinazolinediones
-
Anthranilic acids and alkyl carbazates in refluxing quinoline give high yields of 3-amino-2,4(1H,3H)-quinazolinediones.
- Lalezari, Iraj,Stein, C. A.
-
-
- Tetrazolo[A]quinazol-5-ones antiallergy and antiulcer agents
-
A series of tetrazolo[a]quinazol-5-ones, methods for their production and use as antiallergy agents and antiulcer agents.
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