One‐Pot Synthesis of Functionalized 2,3‐Disubstituted Indolines via K₂CO₃‐Promoted Cascade Michael/Aza‐Cyclization Reactions

Diastereoselective synthesis of trans-2,3-dihydroindoles via formal [4 + 1] annulation reactions of a sulfonium ylide

“…Several cascade approaches have been established utilizing ylide chemistry to access N-heterocycles with remarkable efficiency and selectivity. 10,11,13–18…”

Ethyl 2-[2-(4-Nitrobenzoyl)-1H-indol-3-yl]acetate

“…More than 10,000 biologically active indole derivatives have been identified, and more than 200 derivatives are currently known as pharmaceuticals or undergoing clinical trials [4]. Among the indoles, 2-aroyl indole-3-acetic acid derivatives, which are an important subclass of 2,3-disubstituted indoles [5], have attracted attention as a promising pro-drug for anticancer and antitumor activities [6,7].In continuation of our research interest in 2-aminophenyl α,β-unsaturated carbonyl compounds for the synthesis of highly functionalized indole derivatives [8][9][10], we report here the preparation of a novel ethyl 2-[2-(4-nitrobenzoyl)-1H-indol-3-yl]acetate [11][12][13].…”