- Sequential C-H activation enabled expedient delivery of polyfunctional arenes
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Modular construction of polyfunctional arenes from abundant feedstocks stands as an unremitting pursue in synthetic chemistry, accelerating the discovery of drugs and materials. Herein, using the multiple C-H activation strategy with versatile imidate esters, the expedient delivery of molecular libraries of densely functionalized sulfur-containing arenes was achieved, which enabled the concise construction of biologically active molecules, such as Bipenamol.
- Cai, Xiaoqing,Chen, Qian,Chen, Xiaojian,Gao, Yang,Huo, Yanping,Li, Xianwei,Ouyang, Wensen,Rao, Jianhang,Wang, Jie
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p. 8075 - 8078
(2021/08/20)
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- Method for preparing 2-alkylthiobenzonitrile
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The invention relates to the technical field of fine chemical engineering, and discloses a method for preparing 2-alkylthiobenzonitrile, the method specifically comprises the following steps: taking 2-alkylthiobenzonamide as a raw material and sodium iodide, acetic acid and 1-chloromethyl-4-fluoro-1, 4-diazabicyclo [2.2. 2] octane bis (tetrafluoroborate) [Selectfluor] as additives, reacting in acetonitrile at 120 DEG C for 24 hours, and obtaining the target product 2-alkyl thiobenzonitrile. The method is easy and convenient to operate, reagents and raw materials are easy to obtain, phosphorus oxychloride which is high in toxicity and not easy to store does not need to be used as a dehydrating agent, 2-alkylthiobenzonitrile is efficiently synthesized in one step, and potential application value is achieved.
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Paragraph 0015-0017; 0020
(2022/01/07)
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- Xanthine derivatives, their preparation and use
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The present invention relates to a xanthine derivative, a pharmaceutically acceptable salt thereof, a solvate of the derivative, a solvate of the pharmaceutically acceptable salt, a chemically protected form or prodrug thereof and a preparation method and a use thereof; and also relates to an intermediate compound used for preparing the xanthine derivative and a preparation method of the intermediate compound. The xanthine derivative and a pharmaceutical composition thereof effectively inhibit the activity of DPP-IV, and can be used for preparing a drug for diseases associated with dipeptidyl peptidase (DPP-IV).
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Paragraph 0242-0244
(2017/02/28)
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- Malignant and non-malignant disease treatment with Ras antagonists
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The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival.
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Page/Page column 14
(2016/05/09)
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- MALIGNANT AND NON-MALIGNANT DISEASE TREATMENT WITH RAS ANTAGONISTS
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The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival.
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Paragraph 0070
(2013/04/24)
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- Efficient nickel/N-heterocyclic carbene catalyzed C-S cross-coupling
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The cross-coupling reaction of aryl halides with aliphatic and aromatic thiols catalyzed by readily available Ni(OAc)2 with N-heterocyclic carbene (NHC) is reported. Ni(OAc)2/NHC catalyst showed good activities toward various aryl halides in C-S coupling reaction, even with aryl chlorides. Reactions occurred in excellent yields, broad scope, and high tolerance of functional groups.
- Guan, Pei,Cao, Changsheng,Liu, Yun,Li, Yunfei,He, Pan,Chen, Qian,Liu, Gang,Shi, Yanhui
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supporting information
p. 5987 - 5992,6
(2012/12/12)
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- Efficient nickel/N-heterocyclic carbene catalyzed C-S cross-coupling
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The cross-coupling reaction of aryl halides with aliphatic and aromatic thiols catalyzed by readily available Ni(OAc)2 with N-heterocyclic carbene (NHC) is reported. Ni(OAc)2/NHC catalyst showed good activities toward various aryl halides in C-S coupling reaction, even with aryl chlorides. Reactions occurred in excellent yields, broad scope, and high tolerance of functional groups.
- Guan, Pei,Cao, Changsheng,Liu, Yun,Li, Yunfei,He, Pan,Chen, Qian,Liu, Gang,Shi, Yanhui
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supporting information
p. 5987 - 5992
(2013/01/13)
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- Synthesis and biological evaluation of 2-(3′,4′,5′- trimethoxybenzoyl)-3-aryl/arylaminobenzo[b]thiophene derivatives as a novel class of antiproliferative agents
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The biological importance of microtubules in mitosis, as well as in interphase, makes them an interesting target for the development of anticancer agents. Small molecules such as benzo[b]thiophenes are attractive as inhibitors of tubulin polymerization. T
- Romagnoli, Romeo,Baraldi, Pier Giovanni,Cara, Carlota Lopez,Hamel, Ernest,Basso, Giuseppe,Bortolozzi, Roberta,Viola, Giampietro
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scheme or table
p. 5781 - 5791
(2011/02/22)
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- Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization
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Two new series of inhibitors of tubulin polymerization based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)-benzo[b]thiophene molecular skeleton and its 3-amino positional isomer were synthesized and evaluated for antiproliferative activity, inhibition of tub
- Romagnoli, Romeo,Baraldi, Pier Giovanni,Carrion, Maria Dora,Cara, Carlota Lopez,Preti, Delia,Fruttarolo, Francesca,Pavani, Maria Giovanna,Tabrizi, Mojgan Aghazadeh,Tolomeo, Manlio,Grimaudo, Stefania,Di Cristina, Antonella,Balzarini, Jan,Hadfield, John A.,Brancale, Andrea,Hamel, Ernest
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p. 2273 - 2277
(2008/02/02)
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- Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles
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A new series of compounds, in which the 2-amino-4-methoxyphenyl ring of phenstatin analogue 5 was replaced with 2- or 3-amino-benzoheterocycles, was synthesized and evaluated for antiproliferative activity and inhibition of colchicine binding. The lack of
- Romagnoli, Romeo,Baraldi, Pier Giovanni,Jung, M. Katherine,Iaconinoto, Maria Antonietta,Carrion, Maria Dora,Remusat, Vincent,Preti, Delia,Tabrizi, Mojgan Aghazadeh,Francesca, Fruttarolo,De Clercq, Erik,Balzarini, Jan,Hamel, Ernest
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p. 4048 - 4052
(2007/10/03)
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- Synthesis and analgesic activity of some 1-benzofurans, 1-benzothiophenes and indoles
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3-Unsubstituted 1-benzofurans 1e and 1f, 3-methyl-1-benzofurans 1a-1d, and 3-amino-1-benzofurans 2a-21, as well as 3-amino-1-benzothiophenes 3a, 3b and 3-aminoindoles 4a-4f, 11a, and 11b were prepared and tested as analgesics. The 3-amino-1-benzofurans 2 were prepared from the corresponding 2-hydroxybenzonitriles 5 and phenacyl bromides 6 via intermediates 7. Similar treatment of 2-sulfanylbenzonitrile (8) provided 3-amino-1-benzothiophenes 3. Appropriately substituted 2-aminobenzonitriles 9 then provided N-substituted 3-aminoindoles 4. 1-(Ethoxycarbonyl)indoles 4e and 4f were successfully deprotected giving indoles 11a and 11b, respectively.
- Radl, Stanislav,Hezky, Petr,Urbankova, Jitka,Vachal, Petr,Krejci, Ivan
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p. 280 - 296
(2007/10/03)
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- ETUDE DES REACTIONS DE SRN1-PARTIE 10 ACTION DE SULFANIONS SUR LES HALOGENURES D'ARYLE FONCTIONNALISES. SYNTHESE DIRECTE DE BENZOTHIOPHENES ET THIENOPYRIDINES
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Functionalized aromatic halides Ar1XY (Ar1=C6H4, Y=OCH3,CONH2,CN,COCH3,CHO,COC6H5) undergo SRN1 reactions with sulphur anions -SR, either simple (R=C2H5,CH2C6H5) or functionalized (R=(CH2)2OH,(CH2)2CO2Et,CH2CO2Et).Products Ar1YS- formed from the fragmentation of the radical anion Ar1YSR- are related to the redox potential of the aryl moiety Ar1Y and with the energy of the bond S-R.In the heterocyclic series (Ar2=pyridine, Ar3=quinoline) a similar relationship appears but a competitive SN(AR) reaction occurs for pyridine substrates bearing an electron withdrawing group.A direct synthesis of benzothiophen via SRN1 reaction and an improved synthesis of thienopyridines based on the SN(Ar) reaction are reported.
- Beugelmans, Rene,Bois-Choussy, Michele,Boudet, Bernard
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p. 4153 - 4162
(2007/10/02)
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