- Synthesis of Substituted 4-(Thiophen-2-yl)nicotinonitriles
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Abstract: A series of 4-(thiophen-2-yl)-substituted nicotinonitriles were prepared by a three step procedure including condensation and cyclization of 2-acetylthiophene. A more efficient synthesis of the target products is proposed and the transformation
- Attaryan, H. S.,Hakobyan, R. M.,Hayotsyan, S. S.,Melikyan, G. S.
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- Asymmetric organocatalytic vinylogous Michael addition triggered triple-cascade reactions of 2-hydroxycinnamaldehydes and vinylogous nucleophiles: construction of benzofused oxabicyclo[3.3.1]nonane scaffolds
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An organocatalytic vinylogous Michael addition triggered triple-cascade reaction has been developed. 2-Hydroxycinnamaldehydes worked under iminium activation with either acyclic or cyclic ketone-derived α,α-dicyanoalkenes, yielding the benzofused oxabicyclo[3.3.1]nonanes bearing one quaternary stereocenter with excellent stereoselectivities.
- Wu, Hui-Chun,Wang, Chen,Chen, Ying-Han,Liu, Yan-Kai
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supporting information
p. 1762 - 1765
(2021/02/27)
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- A [5 + 1] annulation strategy for the synthesis of multifunctional biaryls and: P -teraryls from 1,6-Michael acceptor ketene dithioacetals
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A new type of ketene dithioacetal, 2-(3,3-bis-methylsulfanyl-1-arylallylidene)malononitriles containing 1,4 and 1,6-Michael acceptors, were synthesized to study their reactivity for the synthesis of a new molecular entity. We report a [5 + 1] annulation s
- Althagafi, Ismail,Elagamy, Amr,Kumar, Abhinav,Pratap, Ramendra,Shally,Shaw, Ranjay
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p. 6407 - 6417
(2020/09/07)
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- Transition metal free synthesis of multifunctional thiomethylated-benzenes from aryl/heteroaryl/cyclopropyl methyl ketones
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A base-promoted strategic synthesis of various functionalized thiomethylated-benzenes has been established from aryl/heteroaryl/cyclopropyl methyl ketone. We can directly access the thiomethylated-benzene nucleus embedded with diverse functional group by
- Panwar, Rahul,Althagafi, Ismail,Shally,Shaw, Ranjay,Elagamy, Amr,Shah, Chandan,Yadav, Pratik,Pratap, Ramendra
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- "on Water" Direct Catalytic Vinylogous Aldol Reaction of Silyl Glyoxylates
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The unique reactivity of water in the direct catalytic vinylogous aldol reaction of silyl glyoxylates is reported. With the hydrogen-bonding networks from water, the unfavorable homogeneous reactions in organic solvents were severely suppressed, and the "
- Pan, Hong,Han, Man-Yi,Li, Pinhua,Wang, Lei
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p. 14281 - 14290
(2019/11/03)
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- Chemoselective synthesis of m-teraryls through ring transformation of 2 H-pyran-2-ones by 2-(1-arylethylidene)-malononitriles
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We have developed a simple, efficient and chemoselective approach for the synthesis of m-teraryls by the reaction of 6-aryl-2-oxo-4-(sec.amino)-2H-pyran-3-carbonitriles and 2-(1-arylethylidene)malononitriles under basic conditions. We used 6-aryl-2-oxo-4-
- Panwar, Rahul,Shally,Shaw, Ranjay,Elagamy, Amr,Pratap, Ramendra
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p. 8994 - 9002
(2018/12/10)
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- Synthesis and antimicrobial activity of some novel 2-thienyl substituted heterocycles
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A series of 2-thienyl substituted derivatives of thiazoles, oxazoles and spiro(indole-azole) were synthesized. The structures of the synthesized compounds were confirmed by IR, NMR and mass spectral data.
- Youssef, Mohamed Salah K.,Abeed, Ahmed Abdou O.
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- Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors
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Inactivation of the NF-κB signaling pathway by inhibition of IKKβ is a well-known approach to treat inflammatory diseases such as rheumatoid arthritis and cancer. Thienopyrimidine-based analogues were designed through modification of the known IKKβ inhibitor, SPC-839, and then biologically evaluated. The resulting analogues had good inhibitory activity against both nitric oxide and TNF-α, which are well-known inflammatory responses generated by activated NF-κB. However, no inhibitory activity against IKKβ was observed with these compounds. The thienopyrimidine-based analogues were subsequently screened for a target kinase, and FLT3, which is a potential target for acute myeloid leukemia (AML), was identified. Thienopyrimidine-based FLT3 inhibitors showed good inhibition profiles against FLT3 under 1 μM. Overall, these compounds represent a promising family of inhibitors for future development of a treatment for AML.
- Park, Chun-Ho,Lee, Chulho,Yang, Jee Sun,Joe, Bo-Young,Chun, Kwangwoo,Kim, Hyuntae,Kim, Hye Yun,Kang, Jong Soon,Lee, Jangik I.,Kim, Myung-Hwa,Han, Gyoonhee
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p. 2655 - 2660
(2014/06/09)
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- Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors
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Inactivation of the NF-κB signaling pathway by inhibition of IKKβ is a well-known approach to treat inflammatory diseases such as rheumatoid arthritis and cancer. Thienopyrimidine-based analogues were designed through modification of the known IKKβ inhibitor, SPC-839, and then biologically evaluated. The resulting analogues had good inhibitory activity against both nitric oxide and TNF-α, which are well-known inflammatory responses generated by activated NF-κB. However, no inhibitory activity against IKKβ was observed with these compounds. The thienopyrimidine-based analogues were subsequently screened for a target kinase, and FLT3, which is a potential target for acute myeloid leukemia (AML), was identified. Thienopyrimidine-based FLT3 inhibitors showed good inhibition profiles against FLT3 under 1 μM. Overall, these compounds represent a promising family of inhibitors for future development of a treatment for AML.
- Park, Chun-Ho,Lee, Chulho,Yang, Jee Sun,Joe, Bo-Young,Chun, Kwangwoo,Kim, Hyuntae,Kim, Hye Yun,Kang, Jong Soon,Lee, Jangik I.,Kim, Myung-Hwa,Han, Gyoonhee
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p. 2655 - 2660
(2015/02/19)
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- Improved synthesis of mono- and disubstituted 2-halonicotinonitriles from alkylidene malononitriles
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Pyridines with 2,3,4 and/or 5 substitution remain challenging to prepare. Existing strategies to form multisubstituted 2-halonicotinonitriles via enamines suffer from dimerization of the starting alkylidene malononitriles resulting in low yields. Through alteration of reaction conditions, a new high yielding method into enamines was realized by condensing DMF-DMA and alkylidene malononitriles in the presence of substoichiometric acetic anhydride. Cyclization of the resulting enamines under Pinner conditions provided 2-halonicotinonitriles in high overall yields.
- Longstreet, Ashley R.,Campbell, Brian S.,Gupton, B. Frank,McQuade, D. Tyler
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supporting information
p. 5298 - 5301
(2013/11/06)
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- A Simple and Clean Synthesis of Polysubstituted 2,6-Dicyanoanilines Catalyzed by KF/alumina
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A simple and clean synthesis of polysubstituted 2,6-dicyanoanilines has been developed via the reaction of arylidenemalonodinitriles with 1-arylethylidenemalonodinitriles in ethanol catalyzed by KF/ alumina. Use of non-hazardous solid base as a catalyst,
- Jain, Shubha,Keshwal, Balwant S.,Rajguru, Deepika,Bhagwat, Vasant W.
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p. 712 - 715
(2013/03/29)
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- NOVEL THIENOPYRIMIDINE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention relates to a novel thienopyrimidine derivative having an excellent anti? inflammatory and anti-cancer activity, or a pharmaceutically acceptable salt thereof, a process for the preparation thereof and a pharmaceutical composition comprising the same. The compound according to the present invention strongly inhibits IKB kinase-β (IKK-β) involved in the activation of a transcriptional factor, NF-κB, which is associated with inducing various immune and inflammatory diseases, whereby a composition comprising the compound is a useful therapeutic agent against inflammatory diseases, in particular, arthritis and cancer.
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Page/Page column 26; 33
(2010/11/28)
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- New conditions for the synthesis of thiophenes via the Knoevenagel/Gewald reaction sequence. Application to the synthesis of a multitargeted kinase inhibitor
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Novel conditions have been developed for the preparation of substituted 2-aminothiophenes employing the Knoevenagel condensation followed by the Gewald reaction. The benefits of these conditions are their mildness, and the ease of product isolation. Thus,
- Barnes, David M.,Haight, Anthony R.,Hameury, Thomas,McLaughlin, Maureen A.,Mei, Jianzhang,Tedrow, Jason S.,Riva Toma, Joan Dalla
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p. 11311 - 11319
(2007/10/03)
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- Nitriles in Organic Synthesis. The Chemical Behavior of - and malononitriles
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The chemical behavior of - and malononitriles 1a and b toward electrophilic reagents, active methylene reagents and (arylmethylene)malononitriles is described.
- El-Maghraby, Mohamed Abdallah,Sadek, Kamal Usef,Selim, Maghraby Ali,Elnagdi, Mohamed Hilmy
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p. 1375 - 1378
(2007/10/02)
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