1073354-91-2Relevant academic research and scientific papers
Photocatalytic Cross-Couplings of Aryl Halides Enabled by o-Phosphinophenolate and o-Phosphinothiophenolate
Guan, Wei,Li, Runhan,Liu, Can,Shang, Rui,Shen, Ni,Shen, Xuzhong
, p. 2788 - 2795 (2022/02/25)
o-Phosphinophenolate and o-phosphinothiophenolate are potent photocatalysts with strong reducing ability to activate aryl chlorides and bromides under visible light for borylation, arylation, and phosphorylation. Experimental and theoretical studies revealed that the o-diphenylphosphino substituent results in a narrow optical gap and facilitates intersystem crossing to access triplet states, which promote phenolate and thiophenolate to function as effective visible-light-photoredox catalysts. The results presented herein suggest promising utility of synthetically modified phenolates and thiophenolates as photoredox catalysts.
PYRIMIDINE SULFAMIDE DERIVATIVE AND PREPARATION METHOD AND MEDICAL APPLICATION THEREOF
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Paragraph 0282-0284, (2020/09/22)
Disclosed are a series of pyrimidine sulfamide compounds and applications thereof in preparing a drug for a disease related to an ETA receptor antagonist. In particular, disclosed is a derived compound represented by formula (I) or a tautomer or pharmaceutically acceptable composition thereof.
Transformations of Aryl Ketones via Ligand-Promoted C?C Bond Activation
Dai, Hui-Xiong,Li, Hanyuan,Li, Ling-Jun,Liu, Qi-Sheng,Ma, Biao,Wang, Mei-Ling,Wang, Xing,Wang, Zhen-Yu,Xu, Hui
, p. 14388 - 14393 (2020/07/06)
The coupling of aromatic electrophiles (aryl halides, aryl ethers, aryl acids, aryl nitriles etc.) with nucleophiles is a core methodology for the synthesis of aryl compounds. Transformations of aryl ketones in an analogous manner via carbon–carbon bond activation could greatly expand the toolbox for the synthesis of aryl compounds due to the abundance of aryl ketones. An exploratory study of this approach is typically based on carbon–carbon cleavage triggered by ring-strain release and chelation assistance, and the products are also limited to a specific structural motif. Here we report a ligand-promoted β-carbon elimination strategy to activate the carbon–carbon bonds, which results in a range of transformations of aryl ketones, leading to useful aryl borates, and also to biaryls, aryl nitriles, and aryl alkenes. The use of a pyridine-oxazoline ligand is crucial for this catalytic transformation. A gram-scale borylation reaction of an aryl ketone via a simple one-pot operation is reported. The potential utility of this strategy is also demonstrated by the late-stage diversification of drug molecules probenecid, adapalene, and desoxyestrone, the fragrance tonalid as well as the natural product apocynin.
Amino pyrimidine compound and preparation method and application thereof
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Paragraph 0612; 0614; 0655; 0656; 0657; 0658, (2018/11/22)
The invention relates to an amino pyrimidine compound and a preparation method and application thereof. The amino pyrimidine compound has a structure as shown in a formula I. The formula is shown in the description. The compound is an inhibitor of an epidermal growth factor receptor (EGFR) kinase. The invention further relates to a medicine composition comprising the compound, a preparation methodand application thereof in preparation of anti-tumor medicines.
AZABENZIMIDAZOLES AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 86-87, (2011/06/23)
This invention relates to the use of azabenzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of azabenzimidazoles in the treatment of cancer.
IMIDAZOPYRAZINE SYK INHIBITORS
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Page/Page column 92-93, (2010/07/02)
Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample
HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 173-174, (2009/03/07)
The present invention related to novel heterocyclic amide compounds of Formula 1: as disclosed herein or a pharmaceutically accept able salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosedare compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease
