查看更多>>摘要：A simple MCR-Click strategy for the construction of pH-sensitive fluorescent kinase inhibitors by scaffolding a coumarin core with an indole or oxazolone moiety is described. The fluorescent probes thus obtained showed click on fluorescence useful for imaging pH-sensitive tumors, and inhibitor properties against cancer causing cyclin dependent kinase, CDK2. The optical and biological properties observed were rationalized based on DFT calculations and bioassays. The selective binding of these probes with CDK2 and their cytotoxicity towards HeLa cells without affecting normal cells demonstrates that the methodology described here is potentially useful for the design of dual functional probe cum inhibitors for imaging and therapy. (c) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：We have demonstrated a protocol to generalize regioselective 1,2-difunctionalization of alkenes, which is a simple and efficient method for the preparation of haloethers, haloesters and halohydrins using alcohol as nucleophiles with inexpensive and commercially available N-halosuccinimide (NXS) as the halogenat-ing reagent with low catalyst loading under mild reaction condition. The methodology is also applicable for the easy access of various alkenes such as terminal, internal, heterocyclic ones and cyclic endoene with the striking features of high product yields (up to 99%). Moreover, a bioactive molecule was employed as substrate to test this reaction, the corresponding products were successfully prepared with moderate to good yield without losing their ester functional group. The given protocol has the following advantages such as a direct difunctionalization of alkenes, operational simplicity, good functional group tolerance and a wide substrate scope. (c) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：L-proline on multi-wall carbon nanotubes (L-proline/MWCNTs) catalysts doped with suitable auxiliary support materials are successfully applied in the continuous flow catalytic syntheses, including Aldol reaction, Mannich reaction and Knoevenagel condensation reaction. With the advantages of easy operation, high efficiency and excellent stability, this method is promising in large-scale synthesis. (c) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：A transition-metal-free route has been developed for the direct synthesis of biologically significant tetrahydrobenzo[f]quinoline scaffolds. The reaction features polar [4 + 2] Diels-Alder cycloaddition reaction of arynes with a well-designed diene N-Boc protected vinyl tetrahydropyridine, followed by the isomerisation of the double bond leading to the formation of tetrahydrobenzo[f]quinoline scaffolds in good to moderate yields.
查看更多>>摘要：Utilizing simple precursors for the exquisite construction of molecules with diversity and complexity is urgent. Herein, a novel A3-X type reaction for functionalized 3-haloquinolines has been developed by PhI (OAc)2-mediated four-component tandem addition/cyclization/oxidation/aromatization process with simple aromatic amine, aldehyde, alkyne and halide salt. Broad functional group tolerance, very mild condition, easy for further transformation illustrate the concision, high efficiency and practicability of this A3-X type reaction.
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Elsevier