26510-52-1Relevant articles and documents
Design and synthesis of pyridine-pyrazole-sulfonate derivatives as potential anti-HBV agents
Chuang, Hong,Huang, Lin-Chiang Sherlock,Kapoor, Mohit,Liao, Yi-Jen,Yang, Cheng-Lin,Chang, Chia-Ching,Wu, Chun-Yi,Hwu, Jih Ru,Huang, Tsurng-Juhn,Hsu, Ming-Hua
, p. 832 - 836 (2016)
Hepatitis B virus (HBV) is an infectious disease, which can cause acute and chronic infections. Every year, over 7.5 million persons die due to HBV. No effective drug exists for the treatment of HBV. Thus, we designed and synthesized 16 new pyridine-pyraz
Compound, luminescent layer guest material, organic electroluminescent device and display device
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Paragraph 0099-0103; 0112-0116; 0127-0131, (2021/06/22)
The invention provides a compound as shown in a general formula (I). The compoundcan be used for an organic electroluminescent device as a guest material of a luminescent layer. The compound comprises a natural heterocyclic ring and iridium (Ir) coordinated structure, and the light emitting wavelength of the compound can be effectively regulated and controlled. When the compound is used as a guest material of a light-emitting layer, the light-emitting efficiency and the light stability of the organic electroluminescent device can be improved. In addition, the compound provided by the invention is small in molecular weight, is applied to a light-emitting layer, is relatively low in evaporation temperature, and is beneficial to processing. The invention also provides a luminescent layer guest material containing the compound shown in the general formula (I), an organic electroluminescent device and a display device.
Cu-Mediated Expeditious Annulation of Alkyl 3-Aminoacrylates with Aryldiazonium Salts: Access to Alkyl N2-Aryl 1,2,3-Triazole-carboxylates for Druglike Molecular Synthesis
Liu, Hao-Nan,Cao, Hao-Qiang,Cheung, Chi Wai,Ma, Jun-An
supporting information, p. 1396 - 1401 (2020/02/22)
Alkyl N-aryl 1,2,3-triazole-carboxylates are important molecules or intermediates in medicinal chemistry, but the synthesis of N2-aryl counterparts remains elusive. Herein, we describe a Cu-mediated annulation reaction of alkyl 3-aminoacrylates with aryldiazonium salts, both of which are readily available substrates. Furthermore, alkyl 2-aminoacrylates are also viable substrates. Diverse alkyl N2-aryl 1,2,3-triazole-carboxylates and their analogues can be rapidly prepared under mild conditions. Especially, this protocol allows one to access several druglike variants of carbonic anhydrase inhibitors and celecoxib.
6-AMINO-2,4-DIHYDROPYRANO [2,3-C] PYRAZOLES AND METHODS OF USE
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Paragraph 0097-0099; 0101, (2018/10/25)
The present invention generally relates to 6-amino-2,4-dihydropyrano [2,3-c] pyrazoles as a ubiquitin specific protease 7 (USP7) inhibitor useful for the treatment of diseases mediated by malfunction of USP7, such as inflammation, cancer, and immunological disorders. The invention described herein also pertains to pharmaceutical compositions and methods for treating diseases mediated by malfunction of USP7, in mammals using compounds disclosed herein.
The synthesis and evaluation of triazolopyrimidines as anti-tubercular agents
Zuniga, Edison S.,Korkegian, Aaron,Mullen, Steven,Hembre, Erik J.,Ornstein, Paul L.,Cortez, Guillermo,Biswas, Kallolmay,Kumar, Naresh,Cramer, Jeffrey,Masquelin, Thierry,Hipskind, Philip A.,Odingo, Joshua,Parish, Tanya
, p. 3922 - 3946 (2017/07/05)
We identified a di-substituted triazolopyrimidine with anti-tubercular activity against Mycobacterium tuberculosis. Three segments of the scaffold were examined rationally to establish a structure-activity relationship with the goal of improving potency and maintaining good physicochemical properties. A number of compounds displayed sub-micromolar activity against Mycobacterium tuberculosis with no cytotoxicity against eukaryotic cells. Non-substituted aromatic rings at C5 and a two-carbon chain connecting a terminal aromatic at C7 were preferred features; the presence of NH at C7 and a lack of substituent at C2 were essential for potency. We identified compounds with acceptable metabolic stability in rodent and human liver microsomes. Our findings suggest that the easily-synthesized triazolopyrimidines are a promising class of potent anti-tubercular agents and warrant further investigation in our search for new drugs to fight tuberculosis.
Reformatsky and Blaise reactions in flow as a tool for drug discovery. One pot diversity oriented synthesis of valuable intermediates and heterocycles
Huck,Berton,De La Hoz,Díaz-Ortiz,Alcázar
supporting information, p. 1420 - 1424 (2017/05/12)
The application of Reformatsky and Blaise reactions for the preparation of a diverse set of valuable intermediates and heterocycles in a one-pot protocol is described. To achieve this goal, a greener activation protocol for zinc in flow conditions has been developed to introduce this metal efficiently into α-bromoacetates. The organozinc compounds were added to a diverse set of ketones and nitriles to obtain a wide range of functional groups and heterocyclic systems.
Novel Substituted Imidazopyrimidines as Gpbar1 Receptor Modulators
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Paragraph 0115; 0116; 0117; 0133, (2015/05/13)
The present invention relates to novel substituted imidazo[1,2-a]pyrimidine compounds of formula (I), their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present inventio
Facile and short synthesis of (±) 1-hydroxy indolizidine and (±) coniceine from picolinic acid ethyl ester via cross claisen condensation
Veeraswamy,Anjaiah,Yennam, Satyanarayana,Jayashree
, p. 1667 - 1670 (2015/03/04)
New short synthesis of (±) 1-hydroxy indolizidine (4) and (±) coniceine (5) are described starting from picolinic acid ethyl ester (6). The key steps are the conversion of the picolinic acid ethyl ester into β-keto ester 7 via cross Claisen condensation and hydrogenation of the β-keto ester in to hydroxy bicyclic amide (8) using PtO2/H2.
New Pyrazolecarboxylic compd., its manufacturing method and pest control agents
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Paragraph 0129; 0130; 0131, (2018/05/03)
PROBLEM TO BE SOLVED: To provide a new pyrazole compound capable of showing excellent biological activity to not only spider mites but also Nematoda. SOLUTION: It is found that a new pyrazole compound having a nitrogen-containing hetero ring in a first position of a pyrazole ring and a sulfonate group in a fifth position shows excellent biological activity to not only the spider mites but also the Nematoda. COPYRIGHT: (C)2012,JPOandINPIT
Synthesis of pyridyl substituted pyrazolo[4,3-c]pyridines as potential inhibitors of protein kinases
Vilkauskaite, Gyte,Schaaf, Patricia,Saekus, Algirdas,Krystof, Vladimir,Holzer, Wolfgang
, p. 135 - 149 (2014/03/21)
A synthetic route towards 3-(2-pyridyl)-6-(hetero)aryl-1H-pyrazolo[4,3-c] pyridines is described. The key step consists of a microwave-assisted multi-component reaction, including a Sonogashira type cross-coupling of appropriate 5-chloropyrazole-4-carbaldehydes with alkynyl- (hetero)arenes followed by pyridine ring formation of the coupling products in the presence of tert-butylamine, directly affording the title compounds. A congener without substituent at N-1 was accessed via cleavage of a tert-butyl protecting group. Detailed NMR spectroscopic studies (1H, 13C and 15N) were undertaken with the obtained compounds. Selected representatives were evaluated for their potential as inhibitors of protein kinases.