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钯催化Suzuki偶联高效合成2-烷基取代碳青霉烯类衍生物
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【科西医学论文】【摘要】 目的 高效合成多个2-烷基取代碳青霉烯类化合物。方法 通过钯催化下三氟甲磺酰碳青霉烯与烷基硼经由Suzuki偶联高效合成2-烷基取代碳青霉烯化合物。结果 反应合成得到多个目标产物，反应条件温和，收率理想。结论 在合成2-烷基取代碳青霉烯化合物的简便方法中，由于在C-2位引入了烷基链，由此可制备一系列具有临床应用价值的2-烷基取代碳青霉烯类化合物。
【关键词】 钯；碳青霉烯类；Suzuki偶联
Abstract: Objective To synthesize some typical 2-alkylcarbapenems derivatives conveniently. Methods Palladium-catalyzed Suzuki coupling reaction of alkyboranes with carbapenem-2-yl triflates. Results Under mild conditions, the reactions ran smoothly and four 2-alkylcarbapenems derivatives were prepared conveniently in good yield. Conclusion An advantage of this procedure is the introduction of alkyl side chain at C-2 position at the later stage of the synthesis, thus allowing the synthesis of a wide variety of functional 2-alkylcarbapenems more accessible.
Key words: palladium; carbapenems; Suzuki coupling |
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