4101-30-8Relevant academic research and scientific papers
Experimental and Computational Studies on Cp*CyRh(III)/KOPiv-Catalyzed Intramolecular Dehydrogenative Cross-Couplings for Building Eight-Membered Sultam/Lactam Frameworks
Li, Liping,Gao, Hui,Sun, Ming,Zhou, Zhi,Yi, Wei
supporting information, p. 5473 - 5478 (2020/07/14)
Described herein is an unusual Cp*CyRh(III)-catalyzed intramolecular site-specific aryl C-H annulation, a highly chemoselective protocol providing direct access to eight-membered sultams/lactams with broad substrate/functional group tolerance. Experimental and computational studies reveal that such a transformation involves a unique PivOH-assisted aryl C-H activation/alkene insertion/β-H elimination/hydrogen-transfer process involving the Rh(III)-hydride species as the active intermediate with the concomitant release of H2 as the major byproduct, thus enabling the developed Cp*CyRh(III) catalysis with redox-neutral and highly atom-economical features.
Preparation method of intermediate of tyrosine kinase inhibitor
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Paragraph 0022-0033, (2018/11/22)
The invention discloses a preparation method of an intermediate of a tyrosine kinase inhibitor. The preparation method of the intermediate of the tyrosine kinase inhibitor comprises the following steps of allowing a compound II and a compound I to give th
EGFR INHIBITOR, AND PREPARATION AND APPLICATION THEREOF
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, (2017/09/02)
A 4-substituted-2-(N-(5-substituted allyl amide)phenyl)amino)pyrimidine derivative as represented by formula (I), and a preparation and application thereof as an EGFR inhibitor. The compound has activity of inhibiting the L858R EGFR mutant, the T790M EGFR mutant and the exon 19 deletion activating mutant, may be used to treat diseases mediated alone or in part by EGFR mutant activity, and has a wide application in drugs preventing and treating cancers, particularly non-small cell lung cancer.
Photo-Fries rearrangement of aryl acetamides: Regioselectivity induced by the aqueous micellar green environment
Iguchi, Daniela,Erra-Balsells, Rosa,Bonesi, Sergio M.
, p. 105 - 116 (2016/01/20)
Photochemical reactions tend to give more than one photoproduct. However, such a reaction can be a powerful synthetic tool when it is possible to conduct it in regioselective conditions yielding a single photoproduct. Water-surfactant solutions as reaction media can be considered as an approach in this context because they show products with different features than those from isotropic solutions. Here we describe results obtained from studying the effect on the prototypical photoreaction, known as the photo-Fries reaction of several substituted acetanilides and α-naphthyl acetamide within surfactant micelles (ionic and non-ionic micelles). This reaction involves homolytic cleavage of a C-N bond to yield a singlet radical pair. The surfactant micelles control the rotational and translational mobility of the radical pair, resulting in noticeable photoproduct selectivity.
A new general approach to 4-substituted-3-halo-2-quinolones
Zhao, Shuai,He, Yan-hong,Wu, Di,Guan, Zhi
experimental part, p. 597 - 605 (2010/06/21)
A general procedure for the preparation of 4-substituted-3-halo-2-quinolones (halo = F, Cl, Br) utilizing 2-halo diethylphosphonoacetic acids (halo = F, Cl, Br) and o-aminophenylketones as the starting materials is described. The title compounds are obtained by an intramolecular Horner-Wadsworth-Emmons olefination of halogen-containing N-acyl-o-aminophenylketones. The transformation process is generally applicable under mild conditions.
Simple route to 3-(2-indolyl)-1-propanones via a furan recyclization reaction
Butin, Alexander V.,Smirnov, Sergey K.,Stroganova, Tatyana A.,Bender, Wolfgang,Krapivin, Gennady D.
, p. 474 - 491 (2007/10/03)
A simple route to 1-R-3-(2-indolyl)-1-propanones has been elaborated based on recyclization of 2-(2-aminobenzyl)furan derivatives. Being a modification of the Reissert indole synthesis, our approach employs the furan ring as a source of carbonyl function. This approach is general and allows varying of substituents in aromatic ring as well as in 3-position of indole nucleus.
N-[2-CHLORO-4-(6,7-DIMETHOXY-4-QUINOLYL)OXY]PHENYL]-N'-(5-METHYL-3-ISOXAZOLYL)UREA SALT IN CRYSTALLINE FORM
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Page/Page column 18, (2010/02/13)
The present invention provides a crystal of a pharmaceutically acceptable salt of N-{2-chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}-N'-(5-m ethyl-3-isoxazolyl) urea. This crystal of salt is usable for the therapy of a disease selected from the group consisting of tumors, diabetic retinopathy, chronic rheumatism, psoriasis, atherosclerosis, Kaposi's sarcoma, and exudation type age-related maculopathy, and has characteristics suitable for applications of oral pharmaceutical preparations.
Synthesis of condensed quinolines and quinazolines as DNA ligands
Malecki, Natacha,Carato, Pascal,Rigo, Benoit,Goossens, Jean-Francois,Houssin, Raymond,Bailly, Christian,Henichart, Jean-Pierre
, p. 641 - 647 (2007/10/03)
Among new condensed quinolines and quinazolines the design of which were inspired by anti-cancer DNA-binding alkaloids such as camptothecin and batracyclin, DNA binding tests identify the 8-methoxy-7- piperazinylpropoxyindeno[1,2-b]quinolin-11-one tetracyclic system as a new motif for DNA recognition.
5,6-Dialkoxy-3,4-optionally substituted-2(1H)quinazolinones, composition and method of use
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, (2008/06/13)
The synthesis of substituted quinazolinones is described. The novel quinazolinones are renal vasodilators and thereby increase renal blood flow, and are useful as cardiovascular agents.
