Wu Peng, Nielsen Thomas E
Department of Chemistry, Technical University of Denmark, Kongens Lyngby DK-2800, Denmark; Department of Immunology and Microbiology, University of Copenhagen, Copenhagen DK-2200, Denmark; Chemical Biology and Therapeutics Science, Broad Institute of MIT and Harvard, Cambridge, MA 02142, United States; Department of Medicine, Harvard Medical School, Boston, MA 02115, United States; Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, United States; Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA 02139, United States.
Department of Chemistry, Technical University of Denmark, Kongens Lyngby DK-2800, Denmark; Department of Immunology and Microbiology, University of Copenhagen, Copenhagen DK-2200, Denmark; Singapore Centre for Environmental Life Sciences Engineering, Nanyang Technological University, Singapore 637551, Singapore.
Drug Discov Today Technol. 2018 Nov;29:27-33. doi: 10.1016/j.ddtec.2018.06.010. Epub 2018 Jul 17.
The Petasis three-component reaction (PR) of hydroxy aldehydes, amines and boronic acids is an important multi-component reaction for the synthesis of structurally diverse scaffolds and biologically interesting small molecules. The reaction has been significantly explored in the past decade, and many new variants have emerged, such as asymmetric, traceless and four-component approaches. The excellent stereoselectivity, high yield and broad functional group tolerance altogether make this reaction ideal for fragment and compound collection synthesis, since orthogonal chemical handles can be incorporated for subsequent scaffold formation and appendage modification. Herein we present a selection of recent variations on the PR theme for the synthesis of scaffolds of relevance to medicinal chemistry.
羟基醛、胺和硼酸的Petasis三组分反应（PR）是用于合成结构多样的支架和具有生物学意义的小分子的重要多组分反应。在过去十年中，该反应得到了大量研究，出现了许多新的变体，如不对称、无痕和四组分方法。出色的立体选择性、高产率和广泛的官能团耐受性使该反应非常适合片段和化合物库的合成，因为可以引入正交化学手柄用于后续的支架构建和附件修饰。在此，我们展示了一系列基于PR主题的最新变体，用于合成与药物化学相关的支架。
