21930-98-3Relevant academic research and scientific papers
Design, synthesis, and insecticidal activities of novel diamide derivatives with alpha-amino acid subunits
Chen, Rui-Jia,Wang, Jun-Jie,Han, Li,Gu, Yu-Cheng,Xu, Zhi-Ping,Cheng, Jia-Gao,Shao, Xu-Sheng,Xu, Xiao-Yong,Li, Zhong
, p. 1429 - 1436 (2021/05/06)
A series of diamide derivatives containing α-amino acids were designed and synthesized. These compounds were evaluated for their insecticidal activities against Plutella xylostella, Mythimna separate, Myzus persicae, and Tetranychus cinnabarinus. Most of the title compounds containing an l-phenylglycine skeleton were endowed with good activities at the concentration of 500 mg·L?1. Compounds (R)-A6 showed a potential value for further optimization as an insecticidal lead with the LC50 value of 86.8 mg·L?1.
Synthesis of chiral α-amino anilides via a DMEDA-promoted selective C─N coupling reaction of aryl halides and α-aminoamides
Min, Xiangting,Li, Xiaoyu,Wang, Yu,Dong, Yawen,Tang, Jingjing,Wang, Jing,Liu, Jianhui
, p. 2561 - 2566 (2018/04/20)
A DMEDA-promoted and copper-catalyzed approach has been designed for the coupling of aryl halides and chiral α-aminoamides to afford a range of functionalized chiral α-amino anilides. This method has a higher yield and better reproducibility than those under ligand-free conditions. Of the two amino groups in the same molecule, only the amide NH2 is observed to react, showing high regioselectivity. In addition, no racemization occurs, and the ee can reach 99%. For certain hydroxyl-containing substrates, such as L-tyrosine amide and L-threonine amide, addition of a phase transfer catalyst (15-Crown-5) is necessary for such a transformation.
MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF
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Paragraph 00263; 00266; 00267, (2018/11/22)
The present invention provides compounds, compositions thereof, and methods of using the same.
MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF
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Paragraph 0379, (2017/05/15)
The present invention provides compounds, compositions thereof, and methods of using the same.
Synthetic process of chiral N-aromatic amino acid amide
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Paragraph 0010; 0014, (2016/10/17)
Chiral N-aromatic amino acid amide is a core structure fragment of drugs and an intermediate of the drugs. Only if the chiral structure of the product is not required by special raw materials such aryl halide activated by functional groups of nitryl and t
Cysteine protease inhibitors and uses thereof
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Page/Page column 42, (2016/08/29)
The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine
Synthesis of chiral amino acid anilides by ligand-free copper-catalyzed selective N-arylation of amino acid amides
Dong, Junyu,Wang, Yan,Xiang, Qinjie,Lv, Xirui,Weng, Wen,Zeng, Qingle
supporting information, p. 692 - 696 (2013/04/11)
An atom-economic, practical and cost-effective protocol for synthesis of chiral amino acid anilides via ligand-free copper-catalyzed selective C-N cross coupling of chiral amino acid amides and aryl halides, hetereoaryl halides and a vinyl bromide has been developed. No racemization occurred during the C-N coupling. A plausible mechanism is proposed. Copyright
Organocatalysis of asymmetric aldol reaction in water: Comparison of catalytic properties of (S)-valine and (S)-proline amides
Kucherenko,Siyutkin,Dashkin,Zlotin
, p. 1010 - 1015 (2014/03/21)
(S)-Valine amides containing (S)- or (R)-α-phenylethyl substituents at N1 atom efficiently catalyze asymmetric aldol reactions between cyclic (heterocyclic) ketones and aromatic aldehydes in water, predominantly giving rise to the aldol anti-di
Design, synthesis, and optimization of novel epoxide incorporating peptidomimetics as selective calpain inhibitors
Schiefer, Isaac T.,Tapadar, Subhasish,Litosh, Vladislav,Siklos, Marton,Scism, Rob,Wijewickrama, Gihani T.,Chandrasena, Esala P.,Sinha, Vaishali,Tavassoli, Ehsan,Brunsteiner, Michael,Fa', Mauro,Arancio, Ottavio,Petukhov, Pavel,Thatcher, Gregory R. J.
, p. 6054 - 6068 (2013/09/02)
Hyperactivation of the calcium-dependent cysteine protease calpain 1 (Cal1) is implicated as a primary or secondary pathological event in a wide range of illnesses and in neurodegenerative states, including Alzheimer's disease (AD). E-64 is an epoxide-containing natural product identified as a potent nonselective, calpain inhibitor, with demonstrated efficacy in animal models of AD. By use of E-64 as a lead, three successive generations of calpain inhibitors were developed using computationally assisted design to increase selectivity for Cal1. First generation analogues were potent inhibitors, effecting covalent modification of recombinant Cal1 catalytic domain (Cal1cat), demonstrated using LC-MS/MS. Refinement yielded second generation inhibitors with improved selectivity. Further library expansion and ligand refinement gave three Cal1 inhibitors, one of which was designed as an activity-based protein profiling probe. These were determined to be irreversible and selective inhibitors by kinetics studies comparing full length Cal1 with the general cysteine protease papain.
CATALYST FOR ASYMMETRIC HYDROGENATION AND METHOD FOR MANUFACTURING OPTICALLY ACTIVE CARBONYL COMPOUND USING THE SAME
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, (2012/06/16)
The present invention provides a catalyst used for manufacturing an optically active carbonyl compound by selective asymmetric hydrogenation of an α,β-unsaturated carbonyl compound, which is insoluble in a reaction mixture, and a method for manufacturing the corresponding optically active carbonyl compound. Particularly, the invention provides a catalyst for obtaining an optically active citronellal useful as a flavor or fragrance, by selective asymmetric hydrogenation of citral, geranial or neral. The invention relates to a catalyst for asymmetric hydrogenation of an α,β-unsaturated carbonyl compound, which comprises: a powder of at least one metal selected from metals belonging to Group 8 to Group 10 of the Periodic Table, or a metal-supported substance in which the at least one metal is supported on a support; an optically active peptide compound; and an acid, and also relates to a method for manufacturing an optically active carbonyl compound using the same.
