- Asymmetric pyrene derivatives comprising amine group including heteroaryl group and organic light-emitting diode including the same
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The present invention relates to a pyrene derivative represented by [chemical formula A] or [chemical formula B], and an organic light emitting diode comprising the same, wherein substituents Py_1, Py_2, Ar_1, Ar_2, Z, and m are defined in the detailed de
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Paragraph 0379; 0384-0387; 0397; 0406-0409
(2020/11/24)
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- Palladium-catalyzed remote C-H functionalization of 2-aminopyrimidines
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A straightforward strategy was developed for the arylation and olefination at the C5-position of the N-(alkyl)pyrimidin-2-amine core with readily available aryl halides and alkenes, respectively. This approach was highly regioselective, and the transformation was achieved based on two different (Pd(ii)/Pd(iv)) and (Pd(0)/Pd(ii)) catalytic cycles.
- Das, Animesh,Jana, Akash,Maji, Biplab
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supporting information
p. 4284 - 4287
(2020/04/27)
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- CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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Paragraph 0672
(2018/04/17)
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- The Dimroth rearrangement as a probable cause for structural misassignments in imidazo[1,2-a]pyrimidines: A 15N-labelling study and an easy method for the determination of regiochemistry
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Structural misassignments are often seen for complex natural products, but this can also be an issue with seemingly simpler structures. In this paper, we describe how, using a 15N-labelled analogue, we established that the Dimroth rearrangement
- Chatzopoulou, Maria,Martínez, R. Fernando,Willis, Nicky J.,Claridge, Timothy D.W.,Wilson, Francis X.,Wynne, Graham M.,Davies, Stephen G.,Russell, Angela J.
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p. 5280 - 5288
(2018/07/21)
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- Aminoguanidine hydrazone derivatives as non-peptide NPFF1 receptor antagonists reverse opioid induced hyperalgesia
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Neuropeptide FF receptors (NPFF1R and NPFF2R) and their endogenous ligand Neuropeptide FF have been shown previously to display anti-opioid properties and to play a critical role in the adverse effects associated with chronic administrations of opiates including the development of opioid-induced hyperalgesia and analgesic tolerance. In this work, we sought to identify novel NPFF receptors ligands by focusing our interest on a series of heterocycles as rigidified non-peptide NPFF receptor ligands, starting from already described aminoguanidine hydrazones (AGH's). Binding experiments and functional assays highlighted AGH 1n and its rigidified analog 2-amino-dihydropyrimidine 22e for in vivo experiments. As earlier shown with the prototypical dipeptide antagonist RF9, both 1n and 22e reduced significantly the long lasting fentanyl-induced hyperalgesia in rodents. Altogether these data indicate that AGH rigidification maintains nanomolar affinities for both NPFF receptors, while improving antagonist character towards NPFF1R.
- Hammoud, Hassan,Elhabazi, Khadija,Quillet, Rapha?lle,Bertin, Isabelle,Utard, Valérie,Laboureyras, Emilie,Bourguignon, Jean-Jacques,Bihel, Frederic,Simonnet, Guy,Simonin, Frederic,Schmitt, Martine
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- Probing the Scope of the Amidine–1,2,3-triazine Cycloaddition as a Prospective Click Ligation Method
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Despite recent achievements in the development of chemical reactions enabling selective modification of complex biomolecules, the demand for fast and efficient methodologies that allow the attachment of various functional groups to these systems is the subject of intense research. Here, we report on the study of the amidine–1,2,3-triazine cycloaddition reaction, which has the potential to address many of the challenges associated with the development of such chemistry. We describe an optimized protocol leading to the in situ formation of free amidine bases, which directly react in the cycloaddition reaction with 1,2,3-triazines. Our kinetic studies reveal the structural features determining the reaction rates. Finally, we show that the amidine–1,2,3-triazine cycloaddition is extraordinarily selective and orthogonal to other popular ligation reactions. The pros and cons of the methodology are presented.
- Siegl, Sebastian J.,Vrabel, Milan
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supporting information
p. 5081 - 5085
(2018/10/20)
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- Exemplifying Prediction of Preferred Coupling Partners in Developing a Buchwald-Hartwig Coupling for the Synthesis of a c-Kit Inhibitor
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Two convergent syntheses for compound 1 are described that apply Buchwald-Hartwig coupling as the key step. This development work provides a direct comparison of the coupling results from different coupling partners and illustrates that more efficiency ca
- Wu, Quanbing,Xiong, Xin,Cao, Yudong,He, Lijuan,Fei, Zhongbo
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p. 557 - 561
(2018/04/27)
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- 2-polysubstituted aromatic ring-pyrimidine derivative and preparation and medical application
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The invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative, an optical isomer of the derivative or a medically acceptable salt or solvate of the derivative, and application of the compound, the optical isomer of the derivative or the medically acceptable salt or solvate of the derivative in preparing antineoplastic medicine. According to the 2-polysubstituted aromatic ring-pyrimidine derivative, by adopting N-substituted pyridine-2-minopyrimidine as a lead compound obtained based on virtual screening of a structure, a series of brand new small molecule Chk1 inhibitors are designed and synthesized, and a Chk1 kinase inhibitory activity test of a molecular level is conducted on the compound. Experiments prove that the compound is a Chk1 inhibitor with a strong antitumous effect, Chk1 kinase inhibitory activity and a prospect, and new cancer treating medicine, and can be used for treating solid tumor or leukemia related with human or animal cell proliferation. The 2-polysubstituted aromatic ring-pyrimidine derivative has a structure shown in the general formula I.
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Paragraph 0165; 0210; 0217; 0218; 0219
(2017/05/20)
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- ANTIMITOTIC AMIDES FOR THE TREATMENT OF CANCER AND PROLIFERATIVE DISORDERS
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Novel, antimitotic heteroaryl amides and pharmaceutically acceptable salts of Formula I where Ar, R5, R6, R8, R9, R11, X1, and X2 are as defined herein, as compounds for treatment and prevention of cancer and proliferative diseases and disorders.
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Page/Page column 59
(2015/09/28)
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- WNT PATHWAY MODULATORS
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The present invention relates to dihydropyrazolo[l,5-a]pyrimidine compounds of formula I, defined herein, as WNT pathways modulators, processes for making them, and pharmaceutical compositions comprising them. Methods of treatment of conditions mediated by WNT pathway signalling including cancer, fibrosis, stem cell and diabetic retinopathy, rheumatoid arthritis, psoriasis and myocardial infarction, comprising the compounds of formula I are also provided.
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Paragraph 0301; 0302; 0309; 0310
(2015/07/07)
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- Palladium-catalyzed Suzuki cross-coupling of N′-tosyl arylhydrazines
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The first palladium-catalyzed Suzuki cross-coupling of N′-tosyl arylhydrazines with various organoboron reagents has been developed for the preparation of biaryl compounds in high yields. N′-Tosyl arylhydrazine as a readily available and stable electrophile also demonstrated its generality in a number of coupling reactions. The Royal Society of Chemistry 2013.
- Liu, Jin-Biao,Yan, Hui,Chen, Hui-Xuan,Luo, Yu,Weng, Jiang,Lu, Gui
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supporting information
p. 5268 - 5270
(2013/07/04)
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- Studies on Pd/NiFe2O4 catalyzed ligand-free Suzuki reaction in aqueous phase: Synthesis of biaryls, terphenyls and polyaryls
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Palladium supported on nickel ferrite (Pd/NiF2O4) was found to be a highly active catalyst for the Suzuki coupling reaction between various aryl halides and arylboronic acids. The reaction gave excellent yields (70-98%) under ligand free conditions in a 1:1 DMF/H2O solvent mixture, in short reaction times (10-60 min). The catalyst could be recovered easily by applying an external magnetic field. The polyaryls were similarly synthesized.
- Borhade, Sanjay R.,Waghmode, Suresh B.
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experimental part
p. 310 - 319
(2011/06/18)
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- A general and highly efficient method for the construction of aryl-substituted N-heteroarenes
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A general, simple and highly efficient method has been developed for the Pd(OAc)2-catalyzed ligand-free and aerobic Suzuki reaction of N-heteroaryl halides, which is strongly dependent on the molecular structure of solvent. A general, simple and highly efficient method has been developed for the Pd(OAc)2-catalyzed ligand-free and aerobic Suzuki reaction of N-heteroaryl halides including 2-pyridyl bromides, 3-pyridyl bromides, 3-quinolyl bromides, 5-pyrimidyl bromides and 2-pyrazyl chloride, which is strongly dependent on the molecular structure of solvent.
- Liu, Chun,Han, Na,Song, Xiaoxiao,Qiu, Jieshan
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supporting information; experimental part
p. 5548 - 5551
(2011/02/19)
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- Studies on phosphine free Pd-salen complexes as effective catalysts for aqueous Suzuki reaction
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Palladium complexes of the salen ligands, N,N'-bis(salicylidene)- ethylenediamine and N,N'-bis(salicylidene)-1,.-phenylenediamine have been explored for their catalytic activity in a phosphine-free aqueous Suzuki reaction. The various reaction parameters have been systematically optimized with respect to various solvents, bases, temperatures and Pd concentrations. The studies conclude that 1:1 DMF to water solvent ratio, Na2CO 3 as base and 0.5 mo1% of palladium at 90°C is apt for Suzuki reactions. Rapid transformation of substituted aryl iodides and aryl bromides into corresponding biaryls has been observed with excellent yield ranging from 70-86%, under optimized conditions.
- Borhade, Sanjay R.,Waghmode, Suresh B.
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experimental part
p. 565 - 572
(2010/12/25)
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- Titanium catalyzed one-pot multicomponent coupling reactions for direct access to substituted pyrimidines
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A titanium-catalyzed 3-component coupling reaction can be used to generate tautomers of 1,3-diimines. These diimines produced in situ undergo condensation with amidines in a one-pot procedure to provide substituted pyrimidines. Seventeen examples of pyrimidines are provided using this one-pot, 4-component procedure from simple starting materials. In some cases, catalyst architecture can be tuned to control the regioselectivity of the alkyne addition. Finally, the regioselectivity of amidine addition to unsymmetrical 1,3-diimines is discussed.
- Majumder, Supriyo,Odom, Aaron L.
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experimental part
p. 3152 - 3158
(2010/06/11)
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- NITROGENOUS HETEROCYCLIC DERIVATIVE AND ORGANIC ELECTROLUMINESCENT ELEMENT EMPLOYING THE SAME
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A specific derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising the compound. An organic electroluminescence device comprising at least one of organic compound layers including a light emitting layer sandwiched between an anode and a cathode, wherein said at least one of the organic compound layers comprises the derivative of the heterocyclic compound having nitrogen atom as a sole component or as mixed component. The organic electroluminescence device achieves elevation of luminance and excellent efficiency of light emission, and also achieves long lifetime by an improvement of an electrode adhesion.
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Page/Page column 89
(2008/06/13)
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