6135-14-4Relevant academic research and scientific papers
An expedient synthesis of highly functionalized 1,3-dienes by employing cyclopropenes asC4units
Jiang, Chengzhou,Wu, Jiamin,Han, Jiabin,Chen, Kai,Qian, Yang,Zhang, Zhengyu,Jiang, Yaojia
supporting information, p. 5710 - 5713 (2021/06/16)
An efficient method has been described to synthesize dicarbonyl functionalized 1,3-dienes by cleaving the CC bond of enaminones with cyclopropenes in the presence of a rhodium catalyst. The acetate-substituted cyclopropenes are judiciously chosen as standardC4units of 1,3-diene precursors. The reactions are believed to undergo a unique cutting and insertion process, involving a CC bond cleavage of the enaminone and insertion of a newC(sp2) source with the formation of two C-C single bonds. A broad range of substrates can be used to synthesize the corresponding 1,3-dienes under very mild reaction conditions, including low catalyst-loading, ambient temperature, and a neutral reaction solvent.
One-Pot Synthesis of Symmetrical and Asymmetrical 3-Amino Diynes via Cu(I)-Catalyzed Reaction of Enaminones with Terminal Alkynes
Zhang, Changyuan,Guo, Huosheng,Chen, Lulu,Zhang, Jiantao,Guo, Mengping,Zhu, Xuncheng,Shen, Chan,Li, Zeng
supporting information, p. 8169 - 8173 (2021/11/01)
An economical and efficient protocol for the direct construction of amino skipped diynes through the Cu(I)-catalyzed reaction of enaminones and terminal alkynes has been described. Different kinds of symmetrical and asymmetrical 3-amino diynes could be ob
Selective α-Methylation of Ketones
Frolov, Andriy I.,Ostapchuk, Eugeniy N.,Pashenko, Alexander E.,Chuchvera, Yaroslav O.,Rusanov, Eduard B.,Volochnyuk, Dmitriy M.,Ryabukhin, Sergey V.
, p. 7333 - 7346 (2021/06/28)
The convenient and scalable preparative approach for the two-step α-methylation of ketones is described. The optimized protocols for regioselective preparation of enaminones with further diastereoselective and functional groups tolerant hydrogenation to α-methylketones are developed. The scope and limitations of the proposed methodology are discussed. The advantages compared to known procedures are demonstrated. The unexpected role of acetone in the hydrogenation is suggested. The evaluation of the method for both early building block synthesis and late-stage CH-functionalization is shown. The elaborate procedures' preparability and scalability are demonstrated by the synthesis of several α-methyl ketones up to 100 g amount.
Design and evaluation of pyrazolopyrimidines as KCNQ channel modulators
Osuma, Augustine T.,Xu, Xiangdong,Wang, Zhi,Van Camp, Jennifer A.,Freiberg, Gail M.
, (2019/08/13)
Effective treatments of neuropathic pain have been a focus of many discovery programs. KCNQ (kv7) are voltage gated potassium channel openers that have the potential for the treatment of CNS disorders including neuropathic pain. Clinical studies have sugg
Directed C-C bond cleavage of a cyclopropane intermediate generated from: N -tosylhydrazones and stable enaminones: Expedient synthesis of functionalized 1,4-ketoaldehydes
Ni, Meiyan,Zhang, Jianguo,Liang, Xiaoyu,Jiang, Yaojia,Loh, Teck-Peng
supporting information, p. 12286 - 12289 (2017/11/20)
An efficient method to construct functionalized 1,4-ketoaldehydes bearing all-carbon α-quaternary centers via regioselective C-C bond activation has been described. The cyclopropanation of bench-stable enaminones with in situ generated diazo reagents from
Heterocyclic Compounds Useful as RAF Kinase Inhibitors
-
Page/Page column 38, (2009/01/24)
The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
COMPOUNDS USEFUL AS RAF KINASE INHIBITORS
-
Page/Page column 83, (2009/03/07)
The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
PYRIDO PYRIMIDINONES, DIHYDRO PYRIMIDO PYRIMIDINONES AND PTERIDINONES USEFUL AS RAF KINASE INHIBITORS
-
Page/Page column 105, (2010/11/08)
The present invention provides compounds having the formula: (I) wherein A-B together represents one of the following structures; (II), (III), (IV) and n, R1, R2, R3, R4, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., RAF), and thus are useful, for example, for the treatment of RAF mediated diseases.
One-pot synthesis of some 2H-pyran-2-one derivatives
Kepe, Vladimir,Kocevar, Marijan,Polanc, Slovenko
, p. 1707 - 1710 (2007/10/03)
A one-pot synthesis of various 2H-pyran-2-one derivatives 5-19 starting from methyl ketones 1, N,N-dimethylformamide dimethyl acetal and N-acylglycines 3 in acetic anhydride is described.
STUDY OF THE ESCHENMOSER SULFIDE CONTRACTION METHOD WITH AND WITHOUT A THIOPHILE
Corsaro, A.,Perrini, G.,Testa, M. G.,Chiacchio, U.
, p. 197 - 206 (2007/10/02)
Results obtained and observations made by applying the title method for the synthesis of enaminones 5a-o, using triphenylphosphine as a thiophile and triethylamine as a base, are reported.The product distributions of the deprotonations of α-phenacylthio iminium bromides with and without thiophile and those known from thiouronium and heterocyclic thionium analogs are compared.Key words: Enaminones; α-phenacylthio iminium bromides; disulfides; thiiranes.
