Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, Massachusetts 02210, United States.
J Org Chem. 2020 Jul 2;85(13):8732-8739. doi: 10.1021/acs.joc.0c00983. Epub 2020 Jun 16.
A photoredox protocol that uses a heteroleptic Cu (I) complex, [Cu(dq)(BINAP)]BF, has been developed for the photodeprotection of benzenesulfonyl-protected -heterocycles. A range of substrates was examined, including indazoles, indoles, pyrazoles, and benzimidazole, featuring both electron-rich and electron-deficient substituents, giving good yields of the -heterocycle products with broad functional group tolerance. This transformation was also found to be amenable to flow reaction conditions.
一种光氧化还原反应协议，使用了一种异双核铜（I）配合物[Cu(dq)(BINAP)]BF，已被开发用于苯磺酰基保护的杂环的光脱保护。研究了一系列的底物，包括吲哚、苯并咪唑，其中包括富电子和缺电子取代基的吲哚、吡唑，以获得良好的杂环产物收率，并具有广泛的官能团耐受性。这种转化也被发现适用于流动反应条件。
