110802-10-3Relevant academic research and scientific papers
Transition-metal-free oxidative intermolecular cyclization reaction: Synthesis of 2-aryl-4-quinolones
Ma, Haojie,Guo, Cui,Zhan, Zhenzhen,Lu, Guoqiang,Zhang, Yixin,Luo, Xinliang,Cui, Xinfeng,Huang, Guosheng
, p. 5280 - 5283 (2017)
Herein, a novel and efficient intermolecular cyclization of 2-aminoacetophenones with aldehydes was developed for the synthesis of 2-aryl-4-quinolones through C-C and C-N bond formation. Mild conditions, good functional group tolerance, and substrates without prefunctionalization make this protocol practical, and this strategy will stimulate keen interest in fields of chemistry and biology.
QUINOLONE COMPOUNDS AND PROCESS FOR PREPARATION THEREOF
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Paragraph 00047-00048, (2022/03/21)
The present invention relates to quinolones of formula (I) and process for its preparation by amine insertion into aryl-ynones thereof. [Formula I] The invention further relates to the process to obtain the natural products such as: graveoline, graveolinine, pseudane IV, pseudane VII, pseudane VIII and pseudane XII. The invention also describes the process for the total synthesis of waltherione F in concise approach from the quinolone synthesized. [Formula II]
Access to 2-Alkyl/Aryl-4-(1 H)-Quinolones via Orthogonal "nH3" Insertion into o-Haloaryl Ynones: Total Synthesis of Bioactive Pseudanes, Graveoline, Graveolinine, and Waltherione F
Mehta, Goverdhan,Nerella, Sharanya,Pabbaraja, Srihari,Singh, Shweta
, (2020/02/22)
An efficient one-pot synthesis of 4-(1H)-quinolones through an orthogonal engagement of diverse o-haloaryl ynones with ammonia in the presence of Cu(I), involving tandem Michael addition and ArCsp2-N coupling, is presented. The substrate scope of this convenient protocol, wherein ammonium carbonate acts as both an in situ ammonia source and a base toward diverse 2-substituted 4-(1H)-quinolones, has been mapped and its efficacy validated through concise total synthesis of bioactive natural products pseudanes (IV, VII, VIII, and XII), graveoline, graveolinine, and waltherione F.
4-aminoquinoline compound, and preparation method and application thereof
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Paragraph 0032; 0039-0042, (2019/11/12)
The invention discloses a 4-aminoquinoline compound, and a preparation method and application thereof. The second site of the 4-aminoquinoline compound is replaced by cyclic R-base, the 4-aminoquinoline compound is obtained by 4-step reaction of anthranil
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin
Chauhan, Vinita,Chaudhary, Dilip,Pathak, Uma,Saxena, Nandita,Dhaked, Ram Kumar
, p. 10763 - 10773 (2016/12/16)
Shiga toxin (Stx), a category B biothreat agent, is a ribosome inactivating protein and toxic to human and animals. Here, we designed and synthesized small molecules that block the active site of the Stx A subunit. On the basis of binding energy, 20 molec
Direct synthesis of 2-aryl-4-quinolones via transition-metal-free intramolecular oxidative C(sp3)-H/C(sp3)-H coupling
Hu, Wei,Lin, Jian-Ping,Song, Li-Rui,Long, Ya-Qiu
supporting information, p. 1268 - 1271 (2015/05/20)
A novel, metal-free oxidative intramolecular Mannich reaction was developed between secondary amines and unmodified ketones, affording a simple and direct access to a broad range of 2-arylquinolin-4(1H)-ones through C(sp3)-H activation/C(sp3)-C(sp3) bond formation from readily available N-arylmethyl-2-aminophenylketones, using TEMPO as the oxidant and KOtBu as the base.
