钯催化的未活化 C(sp)-H 键间胺化反应合成吲哚啉。
Synthesis of Indolines by Palladium-Catalyzed Intermolecular Amination of Unactivated C(sp)-H Bonds.
机构信息
School of Chemical Science and Engineering, Shanghai Key Laboratory of Chemical Assessment and Sustainability , Tongji University , 1239 Siping Road , Shanghai , 200092 , P. R. China.
出版信息
Org Lett. 2019 Aug 16;21(16):6508-6512. doi: 10.1021/acs.orglett.9b02386. Epub 2019 Aug 5.
A new palladium-catalyzed C(sp)-H amination reaction has been developed. 1-(-Butyl)-2-iodobenzene and its derivatives undergo palladium-catalyzed C-H activation to form palladacycles. The palladacycles are aminated with diaziridinone to form indolines as the final products. The reaction represents a new method for the synthesis of 3,3-disubstituted indolines, which are essential structural motifs in many bioactive compounds and pharmaceutical targets.
一种新的钯催化 C(sp)-H 胺化反应已经被开发出来。1-（-丁基）-2-碘苯及其衍生物经历钯催化的 C-H 活化，形成钯环。钯环与重氮酮发生胺化反应，生成吲哚啉作为最终产物。该反应代表了一种合成 3,3-二取代吲哚啉的新方法，3,3-二取代吲哚啉是许多生物活性化合物和药物靶标中的重要结构基序。
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