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钯催化[4 + 2]环加成方法合成氟化氮杂环。

A Pd-Catalyzed [4 + 2] Annulation Approach to Fluorinated N-Heterocycles.

机构信息

Department of Chemistry, University of Sheffield, Sheffield, S3 7HF, United Kingdom.

Medicinal Chemistry, Oncology R&D Research and Early Development, AstraZeneca Cambridge Science Park, Unit 310 Darwin Building, Cambridge, CB4 0WG, United Kingdom.

出版信息

Org Lett. 2021 Apr 2;23(7):2811-2815. doi: 10.1021/acs.orglett.1c00752. Epub 2021 Mar 24.

Abstract

3-Fluoro- and trifluoromethylthio-piperidines represent important building blocks for discovery chemistry. We report a simple and efficient method to access analogs of these compounds that are armed with rich functionality allowing them to be chemoselectively derivatized with high diastereocontrol.

摘要

3-氟代和三氟甲基硫代哌啶代表了发现化学的重要构建模块。我们报告了一种简单高效的方法来获得这些化合物的类似物,这些类似物具有丰富的功能,可以进行高非对映选择性化学衍生化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e78a/8041373/081dd72511a6/ol1c00752_0001.jpg

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