Straightforward Access to 2-Iodoindolizines via Iodine-Mediated Cyclization of 2-Pyridylallenes,Organic Process Research & Development

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Straightforward Access to 2-Iodoindolizines via Iodine-Mediated Cyclization of 2-Pyridylallenes
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-01-10 , DOI: 10.1021/acs.oprd.9b00418
Thibaut Martinez ₁ , Ismail Alahyen ₁ , Gilles Lemière ₁ , Virginie Mouriès-Mansuy ₁ , Louis Fensterbank ₁

Affiliation

A metal-free access to 2-iodo-1,3-disubstituted indolizines has been developed. The proposed synthesis is relatively simple and efficient and involves the iodine-triggered 5-endo-trig cyclization of 2-pyridylallene precursors. While it can be conducted on a gram scale, the preparation of the precursors is straightforward and does not always require intermediate purifications. The obtained 2-iodoindolizines can be further functionalized through cross-coupling reactions.

中文翻译：

通过碘介导的2-吡啶基烯丙基环化反应，直接获得2-碘吲哚并

已经开发出无金属的2-碘-1,3-二取代的吲哚嗪类药物。拟议的合成相对简单和有效，涉及2-吡啶基丙二烯前体的碘触发的5-内-触发环化。虽然可以以克为单位进行，但前体的制备是直接的，并不总是需要中间纯化。所得的2-碘吲哚并嗪可以通过交叉偶联反应进一步官能化。

更新日期：2020-01-10

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