School of Pharmaceutical Engineering & Life Sciences , Changzhou University , Changzhou 213164 , China.
School of Petrochemical Engineering , Changzhou University , Changzhou 213164 , China.
J Org Chem. 2018 Apr 6;83(7):4257-4263. doi: 10.1021/acs.joc.8b00283. Epub 2018 Mar 21.
An efficient and mild synthesis of a variety of 3-(2-oxopropyl)-isoindolinone derivatives via a BF·EtO catalyzed cascade reaction among 3-hydroxyisoindolin-1-one and phenylacetylene was achieved. Various isoindolinone derivatives were obtained in good to excellent yields. The process, which avoided several drawbacks such as the requirement of concentrated protic acids and metal catalysts, protecting group of nitrogen, high temperature, and multistep synthesis, includes C(sp)-OH cleavage, C-C coupling, and hydration of alkyne.
通过 BF·EtO 催化的 3-羟基异吲哚啉-1-酮与苯乙炔之间的级联反应，实现了各种 3-(2-氧代丙基)-异吲哚啉酮衍生物的高效温和合成。各种异吲哚啉酮衍生物以良好到优秀的产率得到。该过程避免了使用浓质子酸和金属催化剂、氮的保护基、高温以及多步合成等缺点，包括 C(sp)-OH 断裂、C-C 偶联和炔烃的水合反应。
