6526-66-5Relevant academic research and scientific papers
P(III)-Mediated Cascade C-N/C-S Bond Formation: A Protocol towards the Synthesis of N,S-Heterocycles and Spiro Compounds
Polina, Saibabu,Putta, V. P. Rama Kishore,Gujjarappa, Raghuram,Singh, Virender,Pujar, Prasad Pralhad,Malakar, Chandi C.
, p. 431 - 445 (2020/12/07)
A P(III)-mediated entry towards construction of C?N/C?S bond has been devised. The developed heterocyclization method was exercised for the synthesis of a diverse range of N,S-heterocycles and related spiro molecules. P(NMe2)3 revealed the maximum efficacies under the aerobic reaction conditions and a spectrum of bis-nucleophiles, and isothiocyanates were tolerated well to serve the access of manifold immense molecules. (Figure presented.).
Discovery and antitumor activity of Benzo[d]imidazol-containing 2,4-diarylaminopyrimidine analogues as ALK inhibitors with mutation-combating effects
Li, Zheng,Guo, Ming,Cao, Meng,Zhao, Tianming,Li, Mingzhu,Zhai, Xin
, (2021/03/26)
To address drug resistance caused by ALK kinase mutations, a series of novel 2,4-diarylaminopyrimidine (DAAP) analogues were designed by incorporating 1H-benzo[d]imidazol motif onto the maternal framework. All compounds were efficiently synthesized and an
Aromatic heterocycle-containing 2, 4-diarylaminopyrimidine derivative as well as preparation and application of 2, 4-diarylaminopyrimidine derivative
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Paragraph 0322-0324; 0335; 0336, (2020/08/18)
The invention relates to an aromatic heterocycle-containing 2, 4-diarylaminopyrimidine derivative represented by a general formula I, an optical isomer, a pharmaceutically acceptable salt, a solvate or a prodrug thereof, preparation methods of the aromatic heterocycle-containing 2, 4-diarylaminopyrimidine derivative and the optical isomer, the pharmaceutically acceptable salt, the solvate or the prodrug, and a pharmaceutical composition using the compound represented by the general formula I as an active component, wherein substituents R1, R2, R3, R4, R5, R6, X, Y and Z have meanings given inthe specification. The invention also relates to the compound shown in the general formula I, which has strong ALK and ROS1 kinase inhibition effects, and also relates to application of the compound and the optical isomer and pharmaceutically acceptable salt thereof in preparation of drugs for treatment and/or prevention of diseases caused by ALK and ROS1 abnormal expression, and application of the compound in preparation of drugs for prevention of diseases caused by ALK and ROS1 abnormal expression. Use in particular in the preparation of a medicament for treatment and/or for preventing cancer
Facile Access to Amides from Oxygenated or Unsaturated Organic Compounds by Metal Oxide Nanocatalysts Derived from Single-Source Molecular Precursors
Mohammad, Akbar,Chandra, Prakash,Ghosh, Topi,Carraro, Mauro,Mobin, Shaikh M.
, p. 10596 - 10608 (2017/09/12)
Oxidative amidation is a valuable process for the transformation of oxygenated organic compounds to valuable amides. However, the reaction is severely limited by the use of an expensive catalyst and limited substrate scope. To circumvent these limitations, designing a transition-metal-based nanocatalyst via more straightforward and economical methodology with superior catalytic performances with broad substrate scope is desirable. To resolve the aforementioned issues, we report a facile method for the synthesis of nanocatalysts NiO and CuO by the sol-gel-assisted thermal decomposition of complexes [Ni(hep-H)(H2O)4]SO4 (SSMP-1) and [Cu(μ-hep)(BA)]2 (SSMP-2) [hep-H = 2-(2-hydroxylethyl)pyridine; BA = benzoic acid] as single-source molecular precursors (SSMPs) for the oxidative amidation of benzyl alcohol, benzaldehyde, and BA by using N,N-dimethylformamide (DMF) as the solvent and as an amine source, in the presence of tert-butylhydroperoxide (TBHP) as the oxidant, at T = 80 °C. In addition to nanocatalysts NiO and CuO, our previously reported Co/CoO nanocatalyst (CoNC), derived from the complex [CoII(hep-H)(H2O)4]SO4 (A) as an SSMP, was also explored for the aforementioned reaction. Also, we have carefully investigated the difference in the catalytic performance of Co-, Ni-, and Cu-based nanoparticles synthesized from the SSMP for the conversion of various oxygenated and unsaturated organic compounds to their respective amides. Among all, CuO showed an optimum catalytic performance for the oxidative amidation of various oxygenated and unsaturated organic compounds with a broad reaction scope. Finally, CuO can be recovered unaltered and reused for several (six times) recycles without any loss in catalytic activity.
Visible-light photocatalytic α-amino C(sp3)–H activation through radical translocation: a novel and metal-free approach to α-alkoxybenzamides
Huang, Feng-Qing,Dong, Xin,Qi, Lian-Wen,Zhang, Bo
supporting information, p. 1600 - 1604 (2018/03/22)
Visible-light photocatalytic, metal-free synthesis of valuable α-alkoxybenzamides starting with readily prepared o-aminobenzamides and alcohols through radical translocation under mild conditions is reported. This protocol employs eosin Y as an organophot
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.
SUBSTITUTED DIPYRIDO-PYRIMIDO-DIAZEPINE AND BENZO-PYRIDO-PYRIMIDO COMPOUNDS
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Page/Page column 79-80, (2010/10/19)
The present invention relates to substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions contai
ANTHRANILAMIDE INHIBITORS OF AURORA KINASE
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Page/Page column 13, (2008/12/07)
The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; where R1, R2, R3, R4, r and s are as previously defined. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.
Imidazoline derivatives as alpha-1A adrenoceptor ligands
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Page/Page column 18, (2010/02/11)
Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as urinary incontinence.
Dolastatin 15 derivatives
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, (2008/06/13)
Compounds of the present invention include cell growth inhibitors which are peptides of Formula I and acid salts thereof, wherein A, D, and E are α-amino acid residues, B is an α-amino acid residue or an α-hydroxy acid residue, F is an aminobenzoic acid r
