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Synthesis of 3,4-diarylsubstituted hexahydro-1H-indoles
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2018-04-04
Feilong Zhou, Erbao Zhao, Ziqin Yan, Deheng Chen, Yujun Zhao

Efficient syntheses of 3,4-diarylsubstituted hexahydro-1H-indoles in good yields with excellent diastereoselectivities were achieved with a two-step protocol comprising an allylic cation mediated nucleophilic addition and an intramolecular cyclization reaction. The N-aryl sulfonyl protecting groups of cyclization products were readily removed to furnish free amines with retention of halogen substitutions and C-C double bonds.



中文翻译:

3,4-二芳基取代的六氢-1H-吲哚的合成

利用包括烯丙基阳离子介导的亲核加成和分子内环化反应的两步方案,可以高效地合成3,4-二芳基取代的六氢-1H-吲哚并具有出色的非对映选择性。环化产物的N-芳基磺酰基保护基很容易被除去,以提供具有卤素取代和CC双键保留的游离胺。

更新日期:2018-04-06
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