Koning Nicolas R, Strand Daniel
Centre for Analysis and Synthesis, Department of Chemistry, Lund University, Box 124, SE-221 00 Lund, Sweden.
ACS Omega. 2022 Apr 4;7(14):12329-12341. doi: 10.1021/acsomega.2c00810. eCollection 2022 Apr 12.
Synthesis of diketopiperazines has been of long-standing interest in both natural product synthesis and medicinal chemistry. Here, we present an operationally convenient and efficient approach to the fused indoline-diketopiperazine tricyclic core of glionitrin A/B and related structures using a Pd-catalyzed C-H activation reaction to form the indoline five-membered ring. Exploratory work aimed at elaborating the tricyclic structures into the corresponding natural products is discussed.
二酮哌嗪的合成在天然产物合成和药物化学领域一直备受关注。在此，我们报道了一种操作简便且高效的方法，用于合成格利奥尼菌素A/B的稠合吲哚啉-二酮哌嗪三环核心结构及相关结构，该方法利用钯催化的C-H活化反应来形成吲哚啉五元环。文中还讨论了旨在将三环结构进一步转化为相应天然产物的探索性工作。
