Discovery Chemistry , Merck & Co., Inc. , 33 Avenue Louis Pasteur , Boston , Massachusetts 02115 , United States.
Org Lett. 2020 Feb 7;22(3):1052-1055. doi: 10.1021/acs.orglett.9b04587. Epub 2020 Jan 28.
A metallaphotoredox reaction is described that allows for the efficient exploration of benzyl structure-activity relationships on electron-deficient amines. Typically, accessing a variety of benzyl groups on these substrates can be difficult due to the limited availability of the prerequisite building blocks, namely benzyl halides. However, the use of aryl bromides in this metallaphotoredox reaction allows for greater diversity in the benzyl piece. The reaction scope is discussed herein, including conditions for product scaleup using flow.
描述了一种金属光氧化还原反应，可有效地探索缺电子胺上的苄基结构-活性关系。通常，由于所需的前体砌块（即苄基卤化物）的有限可用性，这些底物上的各种苄基基团难以获得。然而，在这种金属光氧化还原反应中使用芳基溴化物可以使苄基部分的多样性更大。本文讨论了反应范围，包括使用流动进行产品放大的条件。
