Synthesis of Anti-inflammatory Agents by Electrochemical Fixation of Carbon Dioxide

1.抗炎药及其前体的合成（1）卤乙烯的电化学羧化反应在常压二氧化碳存在下，以铂为阴极，镁为阳极，在DMF中电解相应的芳基取代溴代乙烯，高产率地制备了2-芳基-2-丙烯酸。2-芳基-2-丙烯酸是各种抗炎剂如布洛芬、萘普生和酮洛芬的前体，实际上通过使用这种电化学羰基化以高产率制备，并且可以通过对映选择性氢化容易地转化为抗炎活性化合物。（2）芳基甲基酮的电化学羧化-类似的芳基甲基酮的电化学羧化以高产率得到2-芳基-2-羟基丙酸，抗炎剂的前体。该方法对洛索洛芬的合成有很好的指导作用。（3）取代苄基卤化物的电化学羧化-Sim ...更多信息 1-芳基-1-卤代乙烷的类似电化学羧化以高产率得到抗炎剂的外消旋混合物。超临界二氧化碳在抗炎药合成中的应用超临界二氧化碳既作为反应试剂又作为反应介质，可以有效地将二氧化碳电化学固定到溴代乙烯、芳基甲基酮和苄基卤上，合成出多种抗炎药.电化学羧化法合成有用羧酸电化学羧化芳基取代的乙烯基三氟甲磺酸酯、脂肪族乙烯基三氟甲磺酸酯和苯基取代的烯烃高产率地合成了相应的α，β-不饱和酸、β-酮基羧酸和2-苯基琥珀酸.微波诱导反应高效立体选择性合成卤代乙烯利用微波诱导反应，在短反应时间内（1-2 min）实现了（E）-和（Z）-卤代乙烯的高效立体选择性合成，它们是合成抗炎药的起始化合物。少

1. Synthesis of Anti-inflammatory Agents and Their Precursors(1)Electrochemical carboxylation of vinyl halides -2-Aryl-2-propenoic acids were prepared in high yields by electrolysis of the corresponding aryl-substituted vinyl bromides in DMF in the presence of atmospheric pressure of carbon dioxide with a platinum cathode and a magnesium anode. 2-Aryl-2-propenoic acids, precursors of various anti-inflammatory agents such as ibuprofen, naproxen, and ketoprofen, were actually prepared in high yields by using this electrochemical carboylation and can readily be transformed into anti-inflammatory active compounds by enantioselectiev hydrogenation.(2)Electrochemical carboxylation of aryl methyl ketones -Similar electrochemical carboxylation of aryl methyl ketones gave 2-aryl-2-hydroxypropanoic acids, precursors of anti-inflammatory agents, in high yields. This method was found to be very useful for a synthesis of loxoprofen.(3)Electrochemical carboxylation of substituted benzyl halides -Sim … More ilar electrochemical carboxylation of 1-aryl-1-haloethanes gave a racemic mixture of anti-inflammatory agents in high yields.2. Use of Supercritical Carbon Dioxide in the Synthesis of Anti-inflammatory AgentsElectrochemical fixation of carbon dioxide to vinyl bromides, aryl methyl ketones, and benzylic halides took place efficiently to give various anti-inflammatory agents when supercritical carbon dioxide was used both as a reagent and-a reaction medium.3. Synthesis of Useful Carboxylic Acids by Electrochemical CarboxylationElectrochemical carboxylation of aryl-substituted vinyl triflates, aliphatic vinyl triflates, and phenyl-substituted alkenes gave the corresponding α, β-unsaturated acids, β-keto carboxylic acids, and 2-phenylsuccinic acids in high yields.4. Highly Efficient and Stereoselective Synthesis of Vinyl Halides by Microwave-induced ReactionHighly efficient and stereoselective synthesis of(E)-and(Z)-vinyl halides, which are starting compounds for a synthesis of anti-inflammatory agents, was achieved in a short reaction time(1-2 min)by using microwave-induced reaction. Less