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首页> 外文期刊>Chemistry: A European journal >Biologically Active Compounds through Catalysis:Efficient Synthesis of N-CHeteroarylcarbony)-N'-(arylalkypiperazines
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Biologically Active Compounds through Catalysis:Efficient Synthesis of N-CHeteroarylcarbony)-N'-(arylalkypiperazines

机译：通过催化生物活性化合物：N-杂芳基碳-N'-（芳基烷基哌嗪）的高效合成

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摘要

A practical route for the synthesis of new biologically active 5-HT_2A receptor antagonists has been developed.In only three catalytic steps,this class of central nervous system(CNS)active compounds can be synthesized efficiently with high diversity.As the initial step,an anti-Markovni-kov addition of amines to styrenes provides an easy route to N-(arylalkyl)pi-perazines,which constitute the core structure of the active molecules.Here,base-catalyzed hydroamination reactions of styrenes with benzylated piper-azine proceeded in high yield even at room temperature.After catalytic de-benzylation,the free amines were successfully carbonylated with different ar-omatic and heteroaromatic halides and carbon monoxide to yield the desired compounds in good to excellent yields.The two key reactions,base-catalyzed hydroamination of styrenes and palladium-catalyzed aminocarbonylation of haloarenes/heterocycles,showed tolerance towards various functional groups,thereby demonstrating the potential to synthesize a wide variety of new derivatives of this promising class of phar-maceuticals.
机译：已开发出一种新的具有生物活性的5-HT_2A受体拮抗剂合成的实用途径。仅需三个催化步骤，就可以高效，高多样性地合成这类中枢神经系统（CNS）活性化合物。胺向苯乙烯的反马可夫尼可夫反加成法提供了一条构成N-（芳基烷基）哌嗪的简便方法，后者构成了活性分子的核心结构。在此，苯乙烯与苄基哌嗪的碱催化加氢胺化反应催化脱苄基反应后，游离胺成功地用不同的芳族和杂芳族卤化物和一氧化碳羰基化，从而以良好或优异的收率得到了所需的化合物。碱催化的加氢胺化是两个关键的反应苯乙烯和钯催化的卤代芳烃/杂环的氨基羰基化反应，显示出对各种官能团的耐受性，从而证明了合成了这一有前途的药理学类别的各种新衍生物。

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