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吲哚烯基取代的嘧啶并[1,2 - ]吲唑类 一种简便的缩合反应。

Indoleninyl-substituted pyrimido[1,2-]indazoles a facile condensation reaction.

作者信息

Ramle Abdul Qaiyum, Fei Chee Chin, Tiekink Edward R T, Basirun Wan Jefrey

机构信息

Department of Chemistry, University of Malaya Kuala Lumpur 50603 Malaysia

Nanotechnology and Catalysis Research Centre, University of Malaya Kuala Lumpur 50603 Malaysia.

出版信息

RSC Adv. 2021 Jul 14;11(40):24647-24651. doi: 10.1039/d1ra04372b. eCollection 2021 Jul 13.

DOI:10.1039/d1ra04372b
PMID:35481028
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9036913/
Abstract

A new series of pyrimido[1,2-]indazoles bearing indolenine moieties was synthesized through a simple condensation reaction with up to 94% yield. The present method features the versatile formation of a pyrimidine ring with a broad range of substrates, great functional group compatibility and facile synthetic operation. The work offers opportunities in drug development as well as in materials science.

摘要

通过简单的缩合反应合成了一系列带有吲哚啉部分的新型嘧啶并[1,2 -]吲唑，产率高达94%。本方法的特点是能与多种底物广泛地形成嘧啶环，具有良好的官能团兼容性且合成操作简便。这项工作为药物开发以及材料科学提供了机会。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/8a39dc4ba948/d1ra04372b-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/c4d979b660a4/d1ra04372b-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/ccef15983779/d1ra04372b-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/d1c6737dd88f/d1ra04372b-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/8a39dc4ba948/d1ra04372b-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/c4d979b660a4/d1ra04372b-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/ccef15983779/d1ra04372b-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/d1c6737dd88f/d1ra04372b-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e0c/9036913/8a39dc4ba948/d1ra04372b-f2.jpg

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本文引用的文献

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Eur J Med Chem. 2021 Jan 1;209:112911. doi: 10.1016/j.ejmech.2020.112911. Epub 2020 Oct 8.
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Aerobic α,β-C(sp)-H Bond Difunctionalization and C-N Bond Cleavage of Triethylamine: Difunctional Ammonium Iodide Enabling the Regioselective Synthesis of 4-Arylpyrimido[1,2-]indazoles.三乙胺的有氧 α,β-C(sp)-H 键双官能化和 C-N 键断裂：双官能化铵碘化盐实现 4-芳基嘧啶并[1,2-a]吲唑的区域选择性合成。
Org Lett. 2019 Aug 2;21(15):6074-6078. doi: 10.1021/acs.orglett.9b02218. Epub 2019 Jul 18.
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Fragment-Based Discovery of Pyrimido[1,2-b]indazole PDE10A Inhibitors.
基于片段的嘧啶并[1,2 - b]吲唑PDE10A抑制剂的发现
Chem Pharm Bull (Tokyo). 2018;66(3):286-294. doi: 10.1248/cpb.c17-00836.
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An approach towards the synthesis of novel fused nitrogen tricyclic heterocyclic scaffolds via GBB reaction.通过 GBB 反应合成新型稠合氮三环杂环骨架的方法。
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