A “One‐Pot” Metal‐Free Synthesis and Evaluation of Antiproliferative Activity of Diversely Functionalized Pyrrolidine‐2‐Ones

A new “one‐pot” metal‐free stereoselective method for the synthesis of diversely functionalized pyrrolidine‐2‐ones from N‐alkyl‐ or N‐arylsulfonamidoacetophenones was developed. The method was used for the synthesis of a new biologically active scaffold with three stereocenters based on diversely functionalized pyrrolidine‐2‐one. The absolute configuration of stereocenters in the new scaffold was established. The novel compounds were obtained with modest to moderate yields. The antiproliferative activities of the new compounds were tested on several cancer cell lines. The majority of the synthesized compounds showed low micromolar antiproliferative activities.