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首页> 外文期刊>Organic letters >Kinetic Resolution of 2?Substituted 2,3-Dihydro-4-pyridones by Palladium-Catalyzed Asymmetric Allylic Alkylation: Catalytic Asymmetric Total Synthesis of Indolizidine (-)-209I
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Kinetic Resolution of 2?Substituted 2,3-Dihydro-4-pyridones by Palladium-Catalyzed Asymmetric Allylic Alkylation: Catalytic Asymmetric Total Synthesis of Indolizidine (-)-209I

机译:钯催化的不对称烯丙基烷基化反应2?取代的2,3-二氢-4-吡啶酮的动力学拆分:吲哚并咪唑(-)-209I的催化不对称全合成

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摘要

The kinetic resolution of 2-substituted-2,3-dihydro-4-pyridones was realized via a Pd-catalyzed allylic substitution reaction using a commercially available (S)-PPhos as a ligand, affording optically active dihydropyridones and C-allylated dihydropyridones in high yields and good enantioselectivities with the S-factor up to 43. With this protocol, a catalytic asymmetric total synthesis of indolizidine (?)-209I was realized for the first time.
机译:通过使用市售的(S)-PPhos作为配体,通过Pd催化的烯丙基取代反应实现2-取代-2,3-二氢-4-吡啶酮的动力学拆分,从而在其中提供光学活性的二氢吡啶酮和C-烯丙基化的二氢吡啶酮。 S因子高达43,具有高收率和良好的对映选择性。通过该方案,首次实现了吲哚并立定(α)-209I的催化不对称全合成。

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