22312-61-4Relevant academic research and scientific papers
Method for reducing aromatic nitro into arylamine
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Paragraph 0169-0172, (2020/07/15)
The invention relates to a method for reducing aromatic nitro to arylamine. The method comprises the following steps: (1) taking an aromatic nitro compound as a raw material, water as a hydrogen source, a palladium compound, cheap and easy to obtain, as a catalyst and tetrahydroxydiboron as an additive to reduce nitro to obtain a product; (2) taking the aromatic nitro compound as the raw material, a copper salt, cheap and easy to obtain, as the catalyst, the tetrahydroxydiboron as the additive to reduce the nitro to obtain a product; and (3) taking the aromatic nitro compound as the raw material, water as the hydrogen source, and the tetrahydroxydiboron as the additive, without needing a metal catalyst, to reduce the nitro to obtain a product. A preparation method for the arylamine, which is provided by the invention, is mild in reaction condition, low in costs, environment-friendly, high in yield, and suitable for industrial production.
Synthesis and biological evaluation of novel benodanil-heterocyclic carboxamide hybrids as a potential succinate dehydrogenase inhibitors
Hou, Taiping,Jiang, Mingfang,Jin, Hong,Tao, Ke,Wan, Jun,Yang, Jian,Zhao, Yongtian
, (2020/10/02)
In order to discover new antifungal agents, twenty novel benodanil-heterocyclic carboxamide hybrids were designed, synthesized, and characterized by 1H NMR and HRMS. In vitro, their antifungal activities against four phytopathogenic fungi were
NaNO2/I2 as an alternative reagent for the synthesis of 1,2,3-benzotriazin-4(3H)-ones from 2-aminobenzamides
Barak, Dinesh S.,Mukhopadhyay, Sushobhan,Dahatonde, Dipak J.,Batra, Sanjay
, p. 248 - 251 (2019/01/04)
An efficient transformation of 2-aminobenzamides to 1,2,3-benzotriazin-4(3H)-ones in the presence of sodium nitrite (NaNO2) and Iodine (I2) is described. The reaction is proposed to proceed via formation of nitrosyl halide that induces nitrosylation of the amino group of 2-aminobenzamide leading to diazotization followed by intramolecular cyclization.
Sulfur-Promoted Synthesis of 2-Aroylquinazolin-4(3H)-ones by Oxidative Condensation of Anthranilamide and Acetophenones
Nguyen, Thanh Binh,Hou, Jing-ya,Retailleau, Pascal
, p. 3337 - 3341 (2019/06/13)
A sulfur-promoted three-component reaction of isatoic anhydride, primary aliphatic or aromatic amines, and acetophenones leading to densely substituted 3-substituted 2-aroylquinazolin-4(3H)-ones is reported. The key step involves a cascade reaction of selective oxidation of the methyl group of the acetophenones, followed by a condensation with anthranilamides. The scope of the reaction is applicable to the synthesis of tryptanthrin and various 3-unsubstituted 2-aroylquinazolin-4(3H)-ones. (Figure presented.).
2 - (2 - Chlorophenyl) quinazoline -4 (3H) - ketone derivative as well as preparation method and application thereof (by machine translation)
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Paragraph 0069; 0074-0076, (2019/08/06)
The invention discloses 2 - (2 - chlorophenyl) quinazoline -4 (3H) - a ketone derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Compared, the traditional Chinese medicinal diazepam, midazolam, and midazolam
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system
Ishihara, Tsukasa,Koga, Yuji,Iwatsuki, Yoshiyuki,Hirayama, Fukushi
, p. 277 - 289 (2015/02/05)
Anticoagulant agents have emerged as a promising class of therapeutic drugs for the treatment and prevention of arterial and venous thrombosis. We investigated a series of novel orally active factor Xa inhibitors designed using our previously reported conjugation strategy to boost oral anticoagulant effect. Structural optimization of anthranilamide derivative 3 as a lead compound with installation of phenolic hydroxyl group and extensive exploration of the P1 binding element led to the identification of 5-chloro-N-(5-chloro-2-pyridyl)-3-hydroxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide (33, AS1468240) as a potent factor Xa inhibitor with significant oral anticoagulant activity. We also reported a newly developed Free-Wilson-like fragment recommender system based on the integration of R-group decomposition with collaborative filtering for the structural optimization process.
Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome
Baugh, Simon D.P.,Pabba, Praveen K.,Barbosa, Joseph,Coulter, Eric,Desai, Urvi,Gay, Jason P.,Gopinathan, Suma,Han, Qiang,Hari, Rajee,Kimball, S. David,Nguyen, Huy V.,Ni, Chi-You,Powell, David R.,Smith, Arian,Terranova, Kristen M.,Wilson, Alan,Yu, Xuan-Chuan,Lombardo, Victoria K.
, p. 3836 - 3839 (2015/08/24)
The synthesis, SAR, and in vivo activity of inhibitors of delta-5 desaturase are described. Ring-constraint of the initial series provided access to a variety of in vitro active chemotypes, from which the indazole was selected. Examples from the indazole
Synthesis, antimicrobial evaluation, ot-QSAR and mt-QSAR studies of 2-amino benzoic acid derivatives
Mahiwal, Kuldeep,Kumar, Pradeep,Narasimhan, Balasubramanian
, p. 293 - 307 (2012/09/07)
A series of 2-amino benzoic acid derivatives (1-28) were synthesized and evaluated for their in vitro antimicrobial activity against the panel of Gram positive, Gram negative bacterial and fungal strains. The results of antimicrobial studies indicated that, in general, the synthesized compounds were found to be bacteriostatic and fungistatic in action. QSAR studies performed by the development of one target and multi target models indicated that multi-target model was effective in describing the antimicrobial activity as well demonstrated the effect of structural parameters viz. LUMO, 3χv and W on antimicrobial activity of 2-amino benzoic acid derivatives. Springer Science+Business Media, LLC 2010.
N-aryl(thio)anthranilic acid amide derivatives, their preparation and their use as VEGF receptor tyrosine kinase inhibitors
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, (2008/06/13)
Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10-(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of
Antithrombotic agents
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, (2008/06/13)
This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
