- THIENOPYRIDINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Since a thienopyridine derivative compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof of the present invention has an excellent effect of inhibiting protein kinase activity, a pharmaceutical composition comprising the same can be usefully used for preventing or treating diseases related to protein kinase activity.COPYRIGHT KIPO 2020
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Paragraph 0228; 0229-0232
(2019/10/29)
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- THIENOPYRIDINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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A thienopyridine derivative compound represented by Formula 1 or pharmaceutically acceptable salts thereof have an excellent inhibitory effect on protein kinase activity, and accordingly, pharmaceutical compositions comprising same can be usefully used for the prevention or treatment of a disease associated with the activity of a protein kinase.
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Page/Page column 30
(2019/10/15)
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- AlCl 3 -Mediated Synthesis of 4-Aryl-2-quinolone-3-carboxylates
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4-Aryl-2-quinolones are important skeletons from both chemical and medicinal viewpoints. We herein report the development of an efficient synthetic method for 3-substituted 4-aryl-2-quinolones. The key reaction in this process involves an AlCl 3/sub
- Yang, Seung-Hye,Jo, Seohyun,Shin, Dongyun
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p. 1614 - 1619
(2017/08/11)
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- Pyranodipyridine Compound
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Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof:
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Paragraph 0326-0328
(2017/06/12)
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- QUINOLINE DERIVATIVE
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This compound represented by general formula (I) and having a quinoline skeleton has a strong Axl inhibitory activity. Consequently, this compound can be a therapeutic agent for Axl-related diseases, for example, cancers such as acute myeloid leukemia, chronic myeloid leukemia, melanoma, breast cancer, pancreatic cancer and glioma, kidney diseases, immune system diseases and cardiovascular diseases.
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Paragraph 0165; 0191
(2017/11/17)
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- Microwave-promoted direct amidation of unactivated esters catalyzed by heteropolyanion-based ionic liquids under solvent-free conditions
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Abstract A simple and efficient procedure for the synthesis of amides directly from unactivated esters and amines catalyzed by heteropolyanion-based ionic liquids under microwave-promoted and solvent-free conditions has been reported. The practical protocol was found to be compatible with different structurally diverse substrates. Moderate to excellent yields, solvent-free media, and operational simplicity are the main highlights. Furthermore, the heteropolyanion-based ionic liquids were easily reusable for this amidation.
- Fu, Renzhong,Yang, Yang,Ma, Yunsheng,Yang, Fei,Li, Jingjing,Chai, Wen,Wang, Quan,Yuan, Rongxin
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supporting information
p. 4527 - 4531
(2015/06/30)
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- Malonic ester amide synthesis: An efficient methodology for synthesis of amides
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A general methodology malonic ester amide synthesis has been demonstrated, which uses α-substituted/unsubstituted diethyl malonates for the decarboxylative acylation of various aromatic/heteroaromatic primary/secondary amines to form one-carbon homologated amides, thus providing easy access to amides with odd/even chain lengths and an array of substituents on the alkyl/aryl part while avoiding use of acyl chlorides or peptide coupling reagents. Copyright
- Mahajan, Pankaj S.,Mahajan, Jyoti P.,Mhaske, Santosh B.
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p. 2508 - 2516
(2013/07/25)
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- Carbene radicals in cobalt(II)-porphyrin-catalysed carbene carbonylation reactions; A catalytic approach to ketenes
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One-pot radicals: Cobalt(III)-carbene radicals, generated by metallo-radical activation of diazo compounds and N-tosylhydrazone sodium salts with cobalt(II) complexes of porphyrins, readily undergo radical addition to carbon monoxide, allowing the catalytic production of ketenes. These ketenes subsequently react with various amines, alcohols and imines in one-pot tandem transformations to produce differently substituted amides, esters and β-lactams in good isolated yields. Copyright
- Paul, Nanda D.,Chirila, Andrei,Lu, Hongjian,Zhang, X. Peter,Debruin, Bas
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supporting information
p. 12953 - 12958
(2013/10/01)
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- Synthesis of carbamoylacetates from α-iodoacetate, CO, and amines under Pd/light combined conditions
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We developed a novel synthetic method of carbamoylacetates from -iodoacetate, carbon monoxide, and amines under photoirradiation conditions in the presence of a Pd catalyst. This reaction likely proceeds via interplay of radical and organopalladium species. Georg Thieme Verlag Stuttgart · New York.
- Sumino, Shuhei,Fusano, Akira,Fukuyama, Takahide,Ryu, Ilhyong
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experimental part
p. 1331 - 1334
(2012/07/13)
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- TMSCL as a rate-accelerating additive in acylations of amines with 5-(α-AMINO-α′-Hydroxy)methylene meldrum acids
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Aspects are presented of the acylation of amines, alcohols, and thiols with 5-(α-amino-α′-hydroxy)methylene Meldrum acids. We placed special emphasis on the acylation reaction of secondary amines with 5-(α-amino-α′-hydroxy)methylene Meldrum acids, which, because of their basicity, caused problems concerning salt formation with a Meldrum acid derivative. We found that secondary amines, which react at the slowest rate and give a poor yield with 5-(α-amino-α′-hydroxy)methylene Meldrum's acid, react quickly and with high yields with the same reagent in the presence 1 to 3 equivalents of TMSCl. Acylation with this derivative of Meldrum acid was optimized for such factors as reaction temperature, solvent polarity, and acidity of the environment. We have prepared a wide range of nonsymmetrical malononic acid diamids, esters, and thioesters of malonamic acid. Taylor & Francis Group, LLC.
- Janikowska, Karolina,Makowiec, Slawomir
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experimental part
p. 975 - 988
(2012/02/03)
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- Pd-catalyzed carbonylation of diazo compounds at atmospheric pressure: A catalytic approach to ketenes
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The carbonylation of carbenes through catalytic cycles is highly desirable due to the importance of ketene-mediated reactions in organic synthesis. In this investigation, a highly efficient and mild catalytic approach toward ketene intermediates has been developed based on Pd-catalyzed carbonylation of diazo compounds with CO. When α-diazocarbonyl compounds or N-tosylhydrazone salts are heated in the presence of a palladium catalyst under atmospheric pressure of CO, ketene intermediates are formed in situ, where they undergo further reactions with various nucleophiles such as alcohols, amines, or imines. The Pd-catalyzed tandem carbonylation-Staudinger cycloaddition gives β-lactam derivatives in good yields with excellent trans diastereoselectivity. The results from DFT calculation on the reaction mechanism suggest that Pd is involved in the [2 + 2] cycloaddition process and affects the diastereoselectivity of the β-lactam products by assisting isomerization of the addition intermediate. On the other hand, the acylketenes generated from the Pd-catalyzed carbonylation of α-diazoketones react with imines in a formal [4 + 2] cycloaddition manner to afford 1,3-dioxin-4-one derivatives. This straightforward carbonylation provides a new approach toward highly efficient catalytic generation of ketene species under mild conditions.
- Zhang, Zhenhua,Liu, Yiyang,Ling, Lin,Li, Yuxue,Dong, Yian,Gong, Mingxing,Zhao, Xiaokun,Zhang, Yan,Wang, Jianbo
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supporting information; experimental part
p. 4330 - 4341
(2011/06/21)
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- AMIDOPHENOXYINDAZOLES USEFUL AS INHIBITORS OF C-MET
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The present invention provides amidophenoxyindazole compounds useful in the treatment of cancer.
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Page/Page column 15
(2010/02/17)
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- PYRIDONE DERIVATIVE AND HERBICIDE
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[Object] To provide a pyridone derivative or an agriculturally acceptable salt thereof which enables control of various weeds growing in upland fields, orchards, paddy fields, and non-crop lands while showing a high safety to useful plants, useful crops,
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Page/Page column 82
(2008/12/04)
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- Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors
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HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. In the search for new IN inhibitors, we designed and synthesized three series of bis-amide and hydrazide-containing derivatives of malonic acid. We performed a docking study to investigate the potential interactions of the title compounds with essential amino acids on the IN active site.
- Sechi, Mario,Azzena, Ugo,Delussu, Maria Paola,Dallocchio, Roberto,Dessi, Alessandro,Cosseddu, Alessia,Pala, Nicolino,Neamati, Nouri
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experimental part
p. 2442 - 2461
(2009/04/05)
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- Nucleophilic substitution accompanying carbon-carbon bond cleavage assisted by a nitro group
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A 2-nitrated 3-oxoester reacted with amines or alcohols to afford unsymmetrical malonic acid derivatives as a result of nucleophilic substitution accompanying C-C bond cleavage. The 2-nitrated 3-oxoester easily formed ammonium salts with amines. When the amine is liberated from the salt under equilibrium, nucleophilic amine and electrophilic keto ester locate close to each other. This intimate pair effect causes a pseudo intramolecular reaction to occur, giving rise to effective substitution under mild conditions.
- Nakaike, Yumi,Taba, Noriko,Itoh, Shinobu,Tobe, Yoshito,Nishiwaki, Nagatoshi,Ariga, Masahiro
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experimental part
p. 2413 - 2417
(2009/09/08)
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- Transacylation of α-Aryl-β-keto Esters
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The acyl group of an α-aryl-β-keto ester was readily transferred to N-, O-, and S-nucleophiles. The transacylation from arylated diethyl 3-oxoglutarate to amines led to unsymmetrical malonic acid amide esters in high yields. The present reaction proceeded under mild conditions without formation of detectable byproducts. Only simple experimental manipulations were required. This reaction was also found to be sensitive to steric factors, which enabled the chemoselective monoacylation of diamines and amino alcohols without any modifications such as protection.
- Nishiwaki, Nagatoshi,Nishida, Daisei,Ohnishi, Tetsuya,Hidaka, Fumie,Shimizu, Satoru,Tamura, Mina,Hori, Kazushige,Tohda, Yasuo,Ariga, Masahiro
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p. 8650 - 8656
(2007/10/03)
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- Efficient synthesis of 4-ethoxycarbonyl pyrazolin-5-one derivatives
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Concise and efficient methods for the preparation of 3-substituted 4-ethoxycarbonylpyrazolin-5-ones are described. The synthetic strategies involve carbon-acylation in the presence of base, followed by ring cyclization with hydrazine or hydrazine monohydrochloride.
- Jung, Jae C.,Watkins, E Blake,Avery, Mitchell A.
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p. 3767 - 3777
(2007/10/03)
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- Reactivity of α-acylated β-enamino ketones and esters: Synthesis of pyrazoles
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The reactivity of the enamino compounds 4-amino-3-phenylamino(thio)carbonyl-3-penten-2-one 1 and 2 and ethyl 3-amino-2-phenylamino(thio)carbonyl-2-butyrate 7 and 8 was studied using the reaction with hydrazine hydrate and hydrazine hydrochloride to evaluate the 1,3 electrophilic center of the compounds by the formation of the pyrazole rings. The pyrazoles 3,4,5,9,11 and 13 were obtained depending on the reaction conditions employed.
- Missio, Lauri J.,Braibante, Hugo S.,Braibante, Mara E. F.
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p. 1243 - 1245
(2007/10/03)
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- The Chemistry of 5-Oxodihydroisoxazoles. XIII. Reactions of the Imino Carbene Derived from Photolysis of Ethyl 5-Oxo-2-phenyl-2,5-dihydroisoxazole-4-carboxylate
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Photolysis of ethyl 5-oxo-2-phenyl-2,5-dihydroisoxazole-4-carboxylate at 300 nm in acetonitrile gives a carbene which is captured efficiently by bromide, chloride, acetate and cyanate, and less efficiently by iodide, thiocyanate, cyclohexene and tetrahydr
- Ang, Kiah H.,Prager, Rolf H.,Williams, Craig M.
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p. 567 - 576
(2007/10/02)
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- Ethyl Esters of Malonanilic Acids. Synthesis and Pyrolysis
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The pyrolysis under 170-220 deg C or boiling in DMF of malonanilic acids ethyl esters (2) is accompanied by formation of malonic acids symmetric dianilides (7) with high yields.A possible mechanism for this transformation has been suggested.
- Ukrainets, Igor V.,Bezugly, Peter A.,Treskach, Vladimir I.,Taran, Svetlana G.,Gorokhova, Olga V.
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p. 10331 - 10338
(2007/10/02)
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- Synthesis of 1,2-Diazetidinones (Aza-β-lactams) by Photochemical Ring Contraction
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Irradiation of 4-diazopyrazolidine-3,5-diones (11) in the presence of alcohols, diethylamine, or water gives 1,2-diazetidinones (12) formed by photochemical Wolff rearrangement with ring contraction followed by reaction of the resulting ketene with the nucleophile.In the case of the bicyclic diazo compound (11d) a fragmentation reaction competes with ring contraction.The aza-β-lactams (12) show the expected high frequency carbonyl stretch in their i.r. spectra.The acid (12e) readily decarboxylates to give the 4-unsubstituted 1,2-dibenzyldiazetidinone (28), the four-membered ring of which is cleaved by alkaline hydrolysis, lithium aluminium hydride or diborane to give (29), (30), and (31), respectively (Scheme 9).Attempts to modify the carboxy substituent of (12e) into an acylamino group were unsuccessful.
- Lawton, Geoffrey,Moody, Christopher J.,Pearson, Christopher J.
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p. 877 - 884
(2007/10/02)
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