709-80-8Relevant academic research and scientific papers
KINASE INHIBITOR
-
Paragraph 0175; 0176, (2021/04/16)
The present invention aims to provide a novel kinase inhibitor and the like, and a therapeutic agent for a disease, a drug discovery screening method and the like utilizing such inhibitor and the like. The compound represented by the following formula (I) and a salt thereof can inhibit plural kinases including LATS (particularly LATS2) which is the major kinase in the Hippo signal transduction pathway. In addition, diseases or tissue damage associated with failure of cellular proliferation can be treated. Therefore, the present invention is beneficial, for example, in the research field of cell functions and diseases, in which the Hippo signal transduction pathway is involved, and the like. Furthermore, it is beneficial in the medical field for the treatment of such diseases and the like. wherein each symbol is as defined in the DESCRIPTION.
Discovery of γ-Lactam alkaloid derivatives as potential fungicidal agents targeting steroid biosynthesis
Cao, Xiufang,Huang, Daye,Huang, Wenbo,Ke, Shaoyong,Song, Di,Wang, Shuangshuang
, p. 14438 - 14451 (2020/12/23)
Biological control of plant pathogens is considered as one of the green and effective technologies using beneficial microorganisms or microbial secondary metabolites against plant diseases, and so microbial natural products have played important roles in the research and development of new and green agrochemicals. To explore the potential applications for natural γ-lactam alkaloids and their derivatives, 26 γ-lactams that have flexible substituent patterns were synthesized and characterized, and their in vitro antifungal activities against eight kinds of plant pathogens belonging to oomycetes, basidiomycetes, and deuteromycetes were fully evaluated. In addition, the high potential compounds were further tested using an in vivo assay against Phytophthora blight of pepper to verify a practical application for controlling oomycete diseases. The potential modes of action for compound D1 against Phytophthora capsici were also investigated using microscopic technology (optical microscopy, scanning electron microscopy, and transmission electron microscopy) and label-free quantitative proteomics analysis. The results demonstrated that compound D1 may be a potential novel fungicidal agent against oomycete diseases (EC50 = 4.9748 μg·mL-1 for P. capsici and EC50 = 5.1602 μg·mL-1 for Pythium aphanidermatum) that can act on steroid biosynthesis, which can provide a certain theoretical basis for the development of natural lactam derivatives as potential antifungal agents.
Copper-catalyzed N–H insertion reactions from sulfoxonium ylides
Furniel, Lucas G.,Burtoloso, Antonio C.B.
, (2020/06/24)
The first use of copper(II) as an efficient catalyst for N–H insertion reactions between anilines and α-carbonyl sulfoxonium ylides is described. Products, 39 arylglycine derivatives, were obtained in yields up to 97% employing a simple and fast experimental procedure.
ADDITIVE COMPOSITION FOR CULTURE MEDIUM, ADDITIVE COMPOUND FOR CULTURE MEDIUM, AND METHOD FOR CULTURE OF CELLS OR TISSUE USING SAME
-
Paragraph 0158-0159, (2020/06/15)
The present invention provides a medium additive composition containing a compound represented by the following formula (I), or a salt thereof: {wherein each symbol is as defined in the DESCRIPTION.}
Method for synthesizing 1,2,3,4-tetrahydroquinoline compounds in mode that decarboxylation of amino acid is catalyzed by visible light
-
Paragraph 0012, (2018/05/30)
The invention relates to a method for synthesizing 1,2,3,4-tetrahydroquinoline compounds in the mode that decarboxylation of amino acid is catalyzed by visible light. The method is characterized in that in an air atmosphere, the N-phenyl amino acidic compounds shown in the formula I, an organic photocatalyst DPZ and 4-molecular sieve are dissolved in an organic solvent, stirred and reacted for atleast 5 hours at the temperature of 20-30 DEG C under the irradiation of the visible light, separation and purification are conducted, and then the tetrahydroquinoline compounds shown in the formula II are obtained, wherein in the formula I and the formula II (the formulas are shown in the description), R is representative for any one of hydrogen, halogen, alkyl, phenyl and alkoxy, R1 is representative for any one of hydrogen, methyl, n-propyl and phenyl, alkyl is representative for methyl or ethyl or normal-butyl or benzyl, and aryl is representative for substituted phenyl or 4-tert-butyl phenyl. According to the method, substrates are simple, reaction conditions are mild, the usage amount of the catalyst is low, the yield is high, and no metal participates in a reaction.
Method for synthesizing 2-(2',6'-dimethylphenyl amino)methyl propionate
-
Paragraph 0005; 0010, (2017/01/12)
The invention discloses a method for synthesizing 2-(2',6'-dimethylphenyl amino)methyl propionate, and belongs to the organic synthesis technical field. L-lactic acid as a starting material is esterified with methanol to obtain L-methyl lactate; then the L-methyl lactate is subjected to a reaction with chlorosulfonic acid under catalysis of concentrated sulfuric acid to generate 2-(3-sulfonylphenyl amino)methyl propionate; next, the 2-(3-sulfonylphenyl amino)methyl propionate is subjected to a reaction with chlorine gas to only generate 2-(2',6'-dichloro-3-sulfonylphenyl amino)methyl propionate, and the reaction yield is improved; then sulfonyl is removed under the action of dilute sulfuric acid; and finally, the obtained product is subjected to a reaction with a Grignard reagent to obtain 2-(2',6'-dimethylphenyl amino)methyl propionate. The method has the advantages of mild and simple operating condition, and the yield is increased and is increased to 91% or more.
A copper-based metal-organic framework as an efficient and reusable heterogeneous catalyst for ullmann and goldberg type C-N coupling reactions
Long, Wei,Qiu, Wenge,Guo, Chongwei,Li, Chuanqiang,Song, Liyun,Bai, Guangmei,Zhang, Guizhen,He, Hong,Kuznetsov, Maxim L.
, p. 21178 - 21192 (2016/01/25)
A highly porous metal-organic framework (Cu-TDPAT), constructed from a paddle-wheel type dinuclear copper cluster and 2,4,6-tris(3,5-dicarboxylphenylamino)-1,3,5-triazine (H6TDPAT), has been tested in Ullmann and Goldberg type C-N coupling reactions of a wide range of primary and secondary amines with halobenzenes, affording the corresponding N-arylation compounds in moderate to excellent yields. The Cu-TDPAT catalyst could be easily separated from the reaction mixtures by simple filtration, and could be reused at least five times without any significant degradation in catalytic activity.
Catalytic enantioselective synthesis of N,Cα,Cα-trisubstituted α-amino acid derivatives using 1H-imidazol-4(5H)-ones as key templates
Etxabe, Julen,Izquierdo, Joseba,Landa, Aitor,Oiarbide, Mikel,Palomo, Claudio
supporting information, p. 6883 - 6886 (2015/06/08)
Abstract 1H-Imidazol-4(5H)-ones are introduced as novel nucleophilic α-amino acid equivalents in asymmetric synthesis. These compounds not only allow highly efficient construction of tetrasubstituted stereogenic centers, but unlike hitherto known templates, provide direct access to N-substituted (alkyl, allyl, aryl) α-amino acid derivatives. A BB method: 1H-imidazol-4(5H)-ones serve as effective and easily available α-amino acid surrogates for the catalytic and highly diastereo- and enantioselective direct construction of N-substituted quaternary α-amino acid derivatives. The reaction is catalyzed by a Br?nsted base (BB) and proceeds with different Michael acceptors. EWG=electron-withdrawing group.
Visible-Light-Mediated 1,2-Acyl Migration: The Reaction of Secondary Enamino Ketones with Singlet Oxygen
Fan, Weigang,Li, Pixu
supporting information, p. 12201 - 12204 (2016/02/23)
Secondary enaminones were oxidized by photochemically generated singlet oxygen, followed by nucleophilic addition of alcohol and an unexpected 1,2-acyl migration to afford quaternary amino acid derivatives. An ene-type reaction pathway is proposed. It is distinctively different from the typical [2+2] addition of singlet oxygen to a C=C bond pathway. Singled out: Secondary enaminones were oxidized by photochemically generated singlet oxygen, and subsequent nucleophilic addition of an alcohol and with an 1,2-acyl migration afforded quaternary amino acid derivatives. An ene-type reaction pathway is proposed. It is distinctively different from the typical [2+2] addition of singlet oxygen to a C=C bond.
Rapid access to α-alkoxy and α-amino acid derivatives through safe continuous-flow generation of diazoesters
Bartrum, Hannah E.,Blakemore, David C.,Moody, Christopher J.,Hayes, Christopher J.
supporting information; experimental part, p. 9586 - 9589 (2011/10/08)
Microreactors: A highly efficient continuous-flow process has been developed for the synthesis of diazoesters from arylsulfonylhydrazones by means of in-flow Bamford-Stevens reactions. Furthermore, a range of α-alkoxy and α-amino acid derivatives have bee
