- Visible light-mediated metal-free double bond deuteration of substituted phenylalkenes
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Various bromophenylalkenes were reductively photodebrominated by using 1,3-dimethyl-2-phenyl-1H-benzo-[d]imidazoline (DMBI) and 9,10-dicyanoanthracene. With deuterated DMBI analogs (the most effective was DMBI-d11), satisfactory to excellent isotopic yields were obtained. DMBI-d11 could also be regenerated from the reaction mixtures with a recovery rate of up to 50%. The combination of the photodebromination reaction with conventional methods for bromoalkene synthesis enables sequential monodeuteration of a double bond without the necessity of a metal catalyst. This journal is
- Iakovenko, Roman,Hlavá?, Jan
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supporting information
p. 440 - 446
(2021/01/28)
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- Modular access to 1,2-allenyl ketones based on a photoredox-catalysed radical-polar crossover process
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Herein, a new protocol dealing with the preparation of 1,2-allenyl ketones has been successfully developedviathe reactions of enynes with radicals enabled by dual photoredox/copper catalysis. Based on the results of a deuteration experiment and the competition reaction between cyclopropanation and allenation, the mechanism based on a photoredox-neutral-catalysed radical-polar crossover process has been proposed. Synthetic applications of allenes have also been demonstrated.
- Du, Chan,Fang, Jianghua,Fang, Yewen,Lei, Wan,Li, Yan,Liu, Yongjun
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supporting information
p. 8502 - 8506
(2021/10/20)
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- New nicotinic acid-based 3,5-diphenylpyrazoles: design, synthesis and antihyperlipidemic activity with potential NPC1L1 inhibitory activity
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Nicotinic acid hydrazide was incorporated into new 4,5-dihydro-5-hydroxy-3,5-diphenylpyrazol-1-yl derivatives. Compounds 6a–h were synthesized, and their antihyperlipidemic activity was evaluated in high cholesterol diet-fed rat model. Compounds 6e, 6f were found to decrease the levels of serum total cholesterol by 14–19% compared to control group. Total triglycerides were also reduced by 24–28% and LDL cholesterol by 16%. As expected from parent niacin, compounds 6e and 6f caused an elevation of HDL cholesterol by 33–41%. Docking study supported the ability of designed compounds to block NPC1L1 active site in a manner similar to that observed with ezetimibe.
- Shoman, Mai E.,Aboelez, Moustafa O.,Shaykhon, Montaser Sh. A.,Ahmed, Sanaa A.,Abuo-Rahma, Gamal El-Din A.,Elhady, Omar M.
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p. 673 - 686
(2020/02/25)
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- Biological evaluation of chalcones and analogues as hypolipidemic agents
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In order to evaluate the anti-hyperlipidemic effect of synthetic chalcones and some analogues, nineteen compounds with different substituents in both rings were synthesized and hypolipidemic activities were measured in vivo using Triton WRl339 acute and hypercaloric chronic assays. 4′,4- dichlorochalcone, 3′,4′,4-trichlorochalcone, and 4′-chlorochalcone gave an excellent decrease in serum total cholesterol and triglycerides in the acute assay. These compounds also showed significant anti-lipidemic activity in the chronic assay.
- Santos, Lorena,Pedrosa, Rozangela Curi,Correa, Rogerio,Cechinel Filho, Valdir,Nunes, Ricardo Jose,Yunes, Rosendo Augusto
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p. 541 - 546
(2007/10/03)
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- Singel-Oxygen Photolysis of Dihaloketones. A Facile and Efficient Approach to Vicinal Triketones and Their Monohydrates
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The preparation of vic-triketones and/or their monohydrates by sensitized photooxidation (singlet oxygen) of gem-dihaloketones and/or vic-dihaloketones is described; some reaction mechanisms are discussed.
- Mahran, M. Refat,Abdou, Wafaa M.,Sidky, Mahmoud M.,Wamhoff, Heinrich
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p. 506 - 508
(2007/10/02)
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