Research and Development, Bristol-Myers Squibb Company , P.O. Box 4000, Princeton, New Jersey 08543-4000 United States.
J Org Chem. 2018 Mar 2;83(5):3000-3012. doi: 10.1021/acs.joc.8b00205. Epub 2018 Feb 14.
An improved, one-pot Minisci reaction has been developed using visible light, an organic photocatalyst, and carboxylic acids as radical precursors via the intermediacy of in situ-generated N-(acyloxy)phthalimides. The conditions employed are mild, demonstrate a high degree of functional group tolerance, and do not require a large excess of the carboxylic acid reactant. As a result, this reaction can be applied to drug-like scaffolds and molecules with sensitive functional groups, enabling late-stage functionalization, which is of high interest to medicinal chemistry.
一种改良的、一锅 Minisci 反应已经开发出来,使用可见光、有机光催化剂和羧酸作为自由基前体,通过原位生成的 N-(酰氧基)邻苯二甲酰亚胺中间体。所采用的条件温和,具有高度的官能团耐受性,并且不需要羧酸反应物的大量过量。因此,该反应可以应用于药物样支架和具有敏感官能团的分子,实现后期的功能化,这对药物化学具有重要意义。