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首页> 外文期刊>Chemistry: A European journal >Direct Synthesis of Highly Substituted Pyrroles and Dihydropyrroles Using Linear Selective Hydroacylation Reactions
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Direct Synthesis of Highly Substituted Pyrroles and Dihydropyrroles Using Linear Selective Hydroacylation Reactions

机译：使用线性选择性加氢酰化反应直接合成高度取代的吡咯和二氢吡咯

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摘要

Rhodium(I) catalysts incorporating small bite-angle diphosphine ligands, such as (Cy2P)(2)NMe or bis(diphenylphosphino)methane (dppm), are effective at catalysing the union of aldehydes and propargylic amines to deliver the linear hydroacylation adducts in good yields and with high selectivities. In situ treatment of the hydroacylation adducts with p-TSA triggers a dehydrative cyclisation to provide the corresponding pyrroles. The use of allylic amines, in place of the propargylic substrates, delivers functionalised dihydropyrroles. The hydroacylation reactions can also be combined in a cascade process with a Rh-I-catalysed Suzuki-type coupling employing aryl boronic acids, providing a three-component assembly of highly substituted pyrroles.
机译：掺入小的咬角二膦配体（例如（Cy2P）（2）NMe或双（二苯基膦基）甲烷（dppm））的铑（I）催化剂可有效催化醛和炔丙基胺的结合，以在其中传递线性加氢加成基产率高，选择性高。用p-TSA原位处理加氢酰化加合物会触发脱水环化反应，从而提供相应的吡咯。使用烯丙基胺代替炔丙基底物可提供官能化的二氢吡咯。加氢酰化反应还可以级联过程与使用芳基硼酸的Rh-I催化的Suzuki型偶联结合，提供高度取代的吡咯的三组分组装。

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