Direct synthesis of fluorinated heteroarylether bioisosteres.

Direct synthesis of fluorinated heteroarylether bioisosteres.
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DOI:
10.1002/anie.201300763
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发表时间:
2013-04-02
影响因子:
16.6
通讯作者:
Baran, Phil S.
Baran, Phil S.
中科院分区:
化学1区
文献类型:
--
作者:
Zhou, Qianghui;Ruffoni, Alessandro;Gianatassio, Ryan;Fujiwara, Yuta;Sella, Eran;Shabat, Doron;Baran, Phil S.

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这项工作描述了一种能够将二氟烷基直接掺入杂环上的试剂的模块化合成方法。该方法的范围和通用性以二氟乙基为例(同时引入了一种新的二氟乙基化试剂 DFES-Na),并为氟化杂芳基醚生物等排体的一般合成提供了原理证明。
This work delineates a method for the modular synthesis of reagents that are capable of direct incorporation of difluoroalkyl groups onto heterocycles. The scope and generality of this method is exemplified with the difluoroethyl group (along with the introduction of a new reagent for difluoroethylation, DFES-Na) and a proof of principle is shown for a general synthesis of fluorinated heteroarylether bioisosteres.
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