Jin Bo, Gopalsamy Ariamala, Peng Bo, Sha Li, Tentarelli Sharon, Gingipalli Lakshmaiah
Medicinal Chemistry, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.
J Org Chem. 2023 Feb 3;88(3):1327-1330. doi: 10.1021/acs.joc.2c01843. Epub 2023 Jan 18.
Herein, we report a photoredox-catalyzed decarboxylative addition of N-substituted acetic acids to aldehydes to generate secondary alcohols under mild reaction conditions. Protic solvents were found to be critical to the successful implementation of this methodology. This strategy enables the formation of a novel C-C bond between aldehydes and N-substituted acetic acid derivatives of weakly nucleophilic and medicinally relevant heteroaryls such as indoles, pyrroles, indazoles, and azaindoles.
在此,我们报道了一种光氧化还原催化的N-取代乙酸与醛的脱羧加成反应,可在温和的反应条件下生成仲醇。发现质子溶剂对于该方法的成功实施至关重要。该策略能够在醛与弱亲核性且具有药物相关性的杂芳基(如吲哚、吡咯、吲唑和氮杂吲哚)的N-取代乙酸衍生物之间形成新型C-C键。