203314-28-7Relevant articles and documents
An Improved Process for the Enantioselective Synthesis of HCV NS5A Inhibitor Elbasvir (MK-8742) Chiral Amine Intermediate
Chapala, Vijaya Lakshmi,Katari, Naresh Kumar,Kerru, Nagaraju,Malavattu, Giri Prasad,Marisetti, Vishnu Murthy,Reddy, Pedavenkatagari Narayana
, p. 932 - 938 (2021/06/26)
Abstract: Large-scale enantioselective synthesis of the chiral amine unit of HCV NS5A inhibitor Elbasvir has been accomplished in six steps, with 55% overall yield. The process includes a highly enantioselective reduction of the NH imine using R-(+)-diphe
Synthetic method for 2,5-dibromophenylacetic acid
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, (2018/03/24)
The invention discloses a synthetic method for an intermediate 2,5-dibromophenylacetic acid of an anti-HCV drug. According to the invention, dibromobenzene is used as a raw material and is subjected to chloromethylation, cyanidation and hydrolysis success
Method for synthesizing 2,5-dibromo phenylacetic acid
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Paragraph 0021; 0022, (2018/12/02)
The invention discloses a method for synthesizing 2,5-dibromo phenylacetic acid. The method comprises the following step: by taking isatin as a raw material, carrying out carbonyl reduction, 5-site bromo reactions and diazotization hydrolysis reactions, thereby obtaining 2,5-dibromo phenylacetic acid, wherein the step of carbonyl reduction is carried out through catalytic hydrogenation reduction;the step of 5-site bromo reactions is carried out with NBS (Bromo-Succinimide) as a bromo agent; and the step of diazotization is carried out with a sodium nitrite/hydrobromic acid system. HBr/cuprousbromide is adopted as a hydrolysis bromo agent. The method has the advantages of being wide in raw material source, mild in reaction condition, high in yield, excellent in quality, low in finished product cost, and the like.
A 2, 5 - di bromo acetic acid
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Paragraph 0018; 0023-0026; 0028; 0033-0036; 0038; 0043-0046, (2017/08/25)
The invention belongs to the technical field of organic chemistry and particularly discloses a method for preparing 2, 5-dibromo-benzene acetic acid. The preparation method comprises the following steps: taking 5-bromoisatin (formula I) as a starting raw material and performing reduction reaction to obtain the bromo-indolone (formula II) and performing diazotized bromization on the bromo-indolone (formula II) to obtain the 2, 5-dibromo-benzene acetic acid (formula III), wherein the reaction process is as follows: FORMULA. By taking the 5-bromoisatin as the starting raw material, the method has the advantages that the 5-bromoisatin is a large-scale produced chemical product with sufficient market supply and low cost.
Synthesis of N-alkoxyindol-2-ones by copper-catalyzed intramolecular N-arylation of hydroxamates
Kukosha, Tatyana,Trufilkina, Nadezhda,Katkevics, Martins
, p. 2525 - 2528 (2011/11/13)
The first example of copper-catalyzed intramolecular N-arylation of hydroxamic acid derivatives is presented. Based on this transformation a new method for the synthesis of N-alkoxyindol-2-ones from 2-(2-bromoaryl) acetylhydroxamates has been developed. T
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity
Szczepankiewicz, Bruce G.,Kosogof, Christi,Nelson, Lissa T. J.,Liu, Gang,Liu, Bo,Zhao, Hongyu,Serby, Michael D.,Xin, Zhili,Liu, Mei,Gum, Rebecca J.,Haasch, Deanna L.,Wang, Sanyi,Clampit, Jill E.,Johnson, Eric F.,Lubben, Thomas H.,Stashko, Michael A.,Olejniczak, Edward T.,Sun, Chaohong,Dorwin, Sarah A.,Haskins, Kristi,Abad-Zapatero, Cele,Fry, Elizabeth H.,Hutchins, Charles W.,Sham, Hing L.,Rondinone, Cristina M.,Trevillyan, James M.
, p. 3563 - 3580 (2007/10/03)
The c-Jun N-terminal kinases (JNK-1, -2, and -3) are members of the mitogen activated protein (MAP) kinase family of enzymes. They are activated in response to certain cytokines, as well as by cellular stresses including chemotoxins, peroxides, and irradiation. They have been implicated in the pathology of a variety of different diseases with an inflammatory component including asthma, stroke, Alzheimer's disease, and type 2 diabetes mellitus. In this work, high-throughput screening identified a JNK inhibitor with an excellent kinase selectivity profile. Using X-ray crystallography and biochemical screening to guide our lead optimization, we prepared compounds with inhibitory potencies in the low-double-digit nanomolar range, activity in whole cells, and pharmacokinetics suitable for in vivo use. The new compounds were over 1000-fold selective for JNK-1 and -2 over other MAP kinases including ERK2, p38α, and p38δ and showed little inhibitory activity against a panel of 74 kinases.
2- and 2,5-substituted phenylketoenols
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Page column 80, (2010/01/31)
The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups ?in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.