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Relevant academic research and scientific papers

6-benzylidene-2-aryl ethynyl cyclohexenone derivative, preparation method and medical applications thereof

The invention discloses 6-benzylidene-2-aryl ethynyl cyclohexenone derivative, a pharmaceutically acceptable salt and a preparation method thereof, a pharmaceutical composition containing the derivative, and medical applications of the derivative and the pharmaceutically acceptable salt, especially applications in preparation of drugs for treating malignant tumors. According to the invention, thecompound has a certain tumor selectivity, can significantly inhibit tumor proliferation, has weak inhibition effect on normal cells, and can significantly inhibit the activity of a TrxR target and induce the increase of the ROS level in tumor cells so as to promote the anti-tumor activity of the compound provided by the invention.

Double Activation Catalysis for α′-Alkylidene Cyclic Enones with Chiral Amines and Thiols

Cooperative catalysis has contributed greatly to the progress of asymmetric synthesis. However, double-activation catalysis has been less explored, especially for covalently tethered species. Here, we present a double-activation strategy for α′-alkylidene cyclic enone substrates that uses a chiral primary amine and 2-mercaptobenzoic acid to promote regio- and chemoselective addition to generate the complex interrupted iminium ion species. Significantly enhanced reactivity and enantioselectivity were observed for β-regioselective Michael addition and Friedel–Crafts alkylation with malononitriles and indoles, respectively, which produced a spectrum of chiral cyclic adducts with an exo-alkylidene group. Moreover, a HRMS study detected a few key covalently tethered intermediates among the substrates and catalysts, which helped elucidate the catalytic mechanism.

Iodotrimethylsilane-Mediated Cross-Aldol Condensation: A Facile Synthesis of α,α′-Bis(substituted benzylidene)cycloalkanones

A facile and efficient method for the preparation of α, α′-bis(substituted benzylidene)cycloalkanones is described for the first time using iodotrimethylsilane generated in situ from chlorotrimethylsilane and sodium iodide in acetonitrile. The reaction proceeds rapidly at room temperature, giving high yields of products.

Synthesis of bis(substituted benzylidene)cycloalkanone using supported reagents and microwave irradiation

Condensation of cycloalkanone with aromatic aldehyde and furfural using supported reagents to prepare bis(substituted benzylidene or furfurylidene)cycloalkanone in excellent yields under microwave irradiation.

UTILIZATION OF PPh3-Ti(IV) REAGENTS. AN EFFICIENT α'-ALKYLIDENATION OF CYCLIC ENONES

PPh3-Ti(IV) reagents can promote regioselective condensation of cyclic enones with aldehydes to give α'-alkylidenecycloenones in good yields.