- REGULATOR OF NITROGEN-CONTAINING HETEROAROMATIC DERIVATIVES, PREPARATION METHOD THEREFOR AND USE THEREOF
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The present invention relates to a regulator of nitrogen-containing heteroaromatic derivatives, a preparation method therefor and the use thereof. In particular, the present invention relates to a compound as shown in the general formula (I), a preparation method therefor and a pharmaceutical composition containing the compound, and the use thereof as a protein tyrosine phosphatase-2C (SHP2) inhibitor in the treatment of diseases or conditions such as leukemia, neuroblastoma, melanoma, breast cancer, lung cancer and colorectal cancer, wherein the definition of each substituent in the general formula (I) is the same as that in the description.
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- Fast and effective reduction of nitroarenes by sodium dithionite under PTC conditions: Application in solid-phase synthesis
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Herein, conditions for the fast and effective reduction of aromatic nitro groups bound to hydrophobic polystyrene-based Wang and Ring resins utilizing sodium dithionite in dichloromethane-water under PTC conditions are reported. Tetrabutylammonium hydrogen sulfate (TBAHS) was found to be an effective phase-transfer catalyst for this reaction. This method allows for the reduction of nitro groups to amino groups under mild conditions with complete conversion and is tolerant of other functional groups. This method is a superior alternative to tin(II) chloride-based reduction, which is known for its shortcomings.
- Kaplánek, Robert,Krchňák, Viktor
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p. 2600 - 2603
(2013/06/05)
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- Potent 2′-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents
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A series of 2′-aminoanilides have been identified which exhibit potent and selective inhibitory activity against the cFMS tyrosine kinase. Initial SAR studies within this series are described which examine aroyl and amino group substitutions, as well as the introduction of hydrophilic substituents on the benzene core. Compound 47 inhibits the isolated enzyme (IC50 = 0.027 μM) and blocks CSF-1-induced proliferation of bone marrow-derived macrophages (IC50 = 0.11 μM) and as such, serves as a lead candidate for further optimization studies.
- Patch, Raymond J.,Brandt, Benjamin M.,Asgari, Davoud,Baindur, Nand,Chadha, Naresh K.,Georgiadis, Taxiarchis,Cheung, Wing S.,Petrounia, Ioanna P.,Donatelli, Robert R.,Chaikin, Margery A.,Player, Mark R.
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p. 6070 - 6074
(2008/03/18)
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