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具有二氟取代侧链的咪唑并[1,2 - ] - 杂环衍生物的制备。

Preparation of imidazo[1,2-]--heterocyclic derivatives with -difluorinated side chains.

作者信息

Hariss Layal, Hadir Kamal Bou, El-Masri Mirvat, Roisnel Thierry, Grée René, Hachem Ali

机构信息

Laboratory for Medicinal Chemistry and Natural Products, Lebanese University, Faculty of Sciences (1) and PRASE-EDST, Hadath, Beirut, Lebanon.

American University of Beirut, Department of Chemistry, Beirut 11-0236, Lebanon.

出版信息

Beilstein J Org Chem. 2017 Oct 10;13:2115-2121. doi: 10.3762/bjoc.13.208. eCollection 2017.

Abstract

Using an aerobic oxidative coupling, different new imidazo[1,2-]--heterocycles with -difluroroalkyl side chains have been prepared in fair yields by the reaction of -difluoroenones with aminopyridines, -pyrimidines and -pyridazines. Condensed heterocycles of this type play an important role as key core structures of various bioactive compounds. Further, starting with a chloroimidazopyridazine derivative, Pd-catalyzed coupling reactions as well as nucleophilic substitutions have been performed successfully in order to increase the molecular diversity.

摘要

通过需氧氧化偶联反应,利用二氟烯酮与氨基吡啶、嘧啶和哒嗪反应,以相当高的产率制备了具有二氟烷基侧链的不同新型咪唑并[1,2 - ] - 杂环。这种类型的稠合杂环作为各种生物活性化合物的关键核心结构发挥着重要作用。此外,从氯代咪唑并哒嗪衍生物出发,成功进行了钯催化的偶联反应以及亲核取代反应,以增加分子多样性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ec5/5647726/753ad825da78/Beilstein_J_Org_Chem-13-2115-g002.jpg

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