63216-04-6Relevant articles and documents
Sequential C-H activation enabled expedient delivery of polyfunctional arenes
Cai, Xiaoqing,Chen, Qian,Chen, Xiaojian,Gao, Yang,Huo, Yanping,Li, Xianwei,Ouyang, Wensen,Rao, Jianhang,Wang, Jie
, p. 8075 - 8078 (2021/08/20)
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.
Method for preparing 2-alkylthiobenzonitrile
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Paragraph 0015-0017; 0020, (2022/01/07)
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.
Xanthine derivatives, their preparation and use
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Paragraph 0242-0244, (2017/02/28)
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).
Malignant and non-malignant disease treatment with Ras antagonists
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Page/Page column 14, (2016/05/09)
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.
MALIGNANT AND NON-MALIGNANT DISEASE TREATMENT WITH RAS ANTAGONISTS
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Paragraph 0070, (2013/04/24)
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.
Efficient nickel/N-heterocyclic carbene catalyzed C-S cross-coupling
Guan, Pei,Cao, Changsheng,Liu, Yun,Li, Yunfei,He, Pan,Chen, Qian,Liu, Gang,Shi, Yanhui
supporting information, p. 5987 - 5992,6 (2012/12/12)
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.
Efficient nickel/N-heterocyclic carbene catalyzed C-S cross-coupling
Guan, Pei,Cao, Changsheng,Liu, Yun,Li, Yunfei,He, Pan,Chen, Qian,Liu, Gang,Shi, Yanhui
supporting information, p. 5987 - 5992 (2013/01/13)
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.
Synthesis and biological evaluation of 2-(3′,4′,5′- trimethoxybenzoyl)-3-aryl/arylaminobenzo[b]thiophene derivatives as a novel class of antiproliferative agents
Romagnoli, Romeo,Baraldi, Pier Giovanni,Cara, Carlota Lopez,Hamel, Ernest,Basso, Giuseppe,Bortolozzi, Roberta,Viola, Giampietro
scheme or table, p. 5781 - 5791 (2011/02/22)
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
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization
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
, p. 2273 - 2277 (2008/02/02)
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
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles
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
, p. 4048 - 4052 (2007/10/03)
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
