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扩展由 - 甲硅烷基芳基三氟甲磺酸酯类前体生成的可合成多取代苯并[]噻吩 6,7 - 噻吩并苯炔。

Expanding the synthesizable multisubstituted benzo[]thiophenes 6,7-thienobenzynes generated from -silylaryl triflate-type precursors.

作者信息

Yoshida Suguru, Kuribara Tomoko, Morita Takamoto, Matsuzawa Tsubasa, Morimoto Kazushi, Kobayashi Takuya, Hosoya Takamitsu

机构信息

Laboratory of Chemical Bioscience, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU) 2-3-10 Kanda-Surugadai, Chiyoda-ku Tokyo 101-0062 Japan

Department of Medical Chemistry and Cell Biology, Graduate School of Medicine, Kyoto University Konoe-cho, Yoshida, Sakyo-ku Kyoto 606-8501 Japan.

出版信息

RSC Adv. 2018 Jun 13;8(39):21754-21758. doi: 10.1039/c8ra04035d.

DOI:10.1039/c8ra04035d
PMID:35541723
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9081209/
Abstract

Various 2,3-disubstituted 6,7-thienobenzynes have been efficiently generated from the corresponding -silylaryl triflate-type precursors by activation with fluoride ions. The method has expanded the scope of synthesizable multisubstituted benzothiophenes, including those with various heteroatom substituents, and can be applied to the synthesis of EP4 antagonist analogs.

摘要

通过氟离子活化，已从相应的硅烷基芳基三氟甲磺酸酯型前体高效生成了各种2,3-二取代的6,7-噻吩并苯炔。该方法扩大了可合成的多取代苯并噻吩的范围，包括那些带有各种杂原子取代基的苯并噻吩，并且可应用于EP4拮抗剂类似物的合成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/10a5a17abc51/c8ra04035d-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/527cb9f5f50e/c8ra04035d-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/75e6581c4d48/c8ra04035d-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/51124b033e1a/c8ra04035d-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/6c38b790f363/c8ra04035d-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/5876e952b6e9/c8ra04035d-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/019787ec61dc/c8ra04035d-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/10a5a17abc51/c8ra04035d-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/527cb9f5f50e/c8ra04035d-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/75e6581c4d48/c8ra04035d-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/51124b033e1a/c8ra04035d-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/6c38b790f363/c8ra04035d-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/5876e952b6e9/c8ra04035d-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/019787ec61dc/c8ra04035d-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05b9/9081209/10a5a17abc51/c8ra04035d-s3.jpg

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