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杂环碘鎓盐作为构建多种多环杂芳烃的通用合成子。

Heterocyclic iodoniums as versatile synthons to approach diversified polycyclic heteroarenes.

作者信息

Zhu Daqian, Wu Zhouming, Liang Liyun, Sun Yameng, Luo Bingling, Huang Peng, Wen Shijun

机构信息

State Key Laboratory of Oncology in South China, Collaborative Innovation Center for Cancer Medicine, Sun Yat-sen University Cancer Center 651 Dongfeng East Road Guangzhou 510060 China

School of Pharmacy, Guangdong Pharmaceutical University 280 Waihuan East Road Guangzhou 510006 China.

出版信息

RSC Adv. 2019 Oct 16;9(57):33170-33179. doi: 10.1039/c9ra07288h. eCollection 2019 Oct 15.

DOI:10.1039/c9ra07288h
PMID:35529157
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9073335/
Abstract

Polycyclic heteroarenes are important scaffolds in the construction of pharmaceuticals. We have previously developed a series of novel heterocyclic iodoniums. In our current work, these unique iodoniums were employed to construct various complex polycyclic heteroarenes with structural diversity tandem dual arylations. As a result, indole, thiophene and triphenylene motifs were fused into these heterocycles with high molecular quality, which might provide promising fragments in drug discovery. Moreover, these heterocycles could be diversified at a late stage.

摘要

多环杂芳烃是药物构建中的重要骨架。我们之前开发了一系列新型杂环碘鎓盐。在我们目前的工作中，这些独特的碘鎓盐被用于通过串联双芳基化构建各种结构多样的复杂多环杂芳烃。结果，吲哚、噻吩和三亚苯基序以高分子质量融合到这些杂环中，这可能为药物发现提供有前景的片段。此外，这些杂环可以在后期实现多样化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/e7da856a6d13/c9ra07288h-s6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/5ca9eb8a8ce2/c9ra07288h-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/9170b3a6fe01/c9ra07288h-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/932601e13dac/c9ra07288h-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/e8c374236ca5/c9ra07288h-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/1f3d0147e611/c9ra07288h-s4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/02cc381b1539/c9ra07288h-s5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/e7da856a6d13/c9ra07288h-s6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/5ca9eb8a8ce2/c9ra07288h-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/9170b3a6fe01/c9ra07288h-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/932601e13dac/c9ra07288h-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/e8c374236ca5/c9ra07288h-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/1f3d0147e611/c9ra07288h-s4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/02cc381b1539/c9ra07288h-s5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0296/9073335/e7da856a6d13/c9ra07288h-s6.jpg

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