نتایج جستجو برای: michael acceptor

تعداد نتایج: 39399  

Journal: :Angewandte Chemie 2022

An antiaromatic molecular propeller acts as a strong electron acceptor, fluorophore, and dye in bulk heterojunction solar cells. In their Research Article (e202212293), Glib V. Baryshnikov, Colin Nuckolls, Michael Pittelkow, co-workers report how annulation of four perylene diimides to tetraoxa[8]circulene gives dynamic non-planar π-conjugated molecule with 32 aromatic rings surrounding central...

2001
Alfred Hassner Eugene Ghera Tamar Yechezkel Victoria Kleiman Thiagarajan Balasubramanian Daryl Ostercamp

Abstract: This lecture describes some of our studies of lithio derivatives of allyl sulfone carbanions which add α-regioselectively as well as anti diastereoselectively to Michael acceptor olefins. This can be ascribed to chelation in the Michael addition step. When the reaction leads to subsequent ring closure by using a bromoallyl sulfone, the latter acts as a methylenemethane synthon in a (3...

2016
Yufeng Miao Pieter G Tepper Edzard M Geertsema Gerrit J Poelarends

The enzyme 4-oxalocrotonate tautomerase (4-OT) promiscuously catalyzes the Michael-type addition of acetaldehyde to β-nitrostyrene derivatives to yield chiral γ-nitroaldehydes, which are important precursors for pharmaceutically active γ-aminobutyric acids. In this study, we investigated the effect of different substituents at the aromatic ring of the Michael acceptor on the catalytic efficienc...

Journal: :Organic & biomolecular chemistry 2011
Denis Mulliner Dominik Wondrousch Gerrit Schüürmann

The electrophilic reactivity of Michael acceptors is an important determinant of their toxicity. For a set of 35 α,β-unsaturated aldehydes, ketones and esters with experimental rate constants of their reaction with glutathione (GSH), k(GSH), quantum chemical transition-state calculations of the corresponding Michael addition of the model nucleophile methane thiol (CH(3)SH) have been performed a...

Journal: :Chemical & pharmaceutical bulletin 2000
K Sato M Tamura K Tamoto M Omote A Ando I Kumadaki

We have reported that the reaction of ethyl bromodifluoroacetate (1) with alkenyl iodides in the presence of copper powder gives ethyl alkenyldifluoroacetates. As an extension of this reaction, reaction of 1 with Michael acceptors in the presence of copper powder was examined and found to give 1,4-addition products selectively, unless the acceptor has a group stabilizing a radical intermediate,...

Journal: :Journal of medicinal chemistry 2010
Chia-Hsien Wu Mohane Selvaraj Coumar Chang-Ying Chu Wen-Hsing Lin Yi-Rong Chen Chiung-Tong Chen Hui-Yi Shiao Shaik Rafi Sing-Yi Wang Hui Hsu Chun-Hwa Chen Chun-Yu Chang Teng-Yuan Chang Tzu-Wen Lien Ming-Yu Fang Kai-Chia Yeh Ching-Ping Chen Teng-Kuang Yeh Su-Huei Hsieh John T-A Hsu Chun-Chen Liao Yu-Sheng Chao Hsing-Pang Hsieh

HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 antiproliferative activity compared to HTS hit 7 and also inhibited gefitinib-resistant double mutant (DM, T790M/L858R) EGFR kinase at nanomola...

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