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jo9b01920_si_002.cif (9.18 MB)

Synthesis of 7′-Arylidenespiro[indoline-3,1′-pyrrolizines] and 7′-Arylidenespiro[indene-2,1′-pyrrolizines] via [3 + 2] Cycloaddition and β‑C–H Functionalized Pyrrolidine

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posted on 2019-09-19, 13:36 authored by Ying Huang, Hui-Lin Fang, Yi-Xin Huang, Jing Sun, Chao-Guo Yan
The acetic acid catalyzed three-component reaction of pyrrolidine, aromatic aldehydes, and 3-arylideneoxindolin-2-ones in refluxing toluene afforded functionalized 7′-arylidenespiro­[indoline-3,1′-pyrrolizines] in good yields and with high diastereoselectivity. The similar three-component reaction with 2-arylidene-1,3-indanediones also gave 7′-arylidenespiro­[indene-2,1′-pyrrolizines] in good yields. However, the reaction with 3-phenacylideneoxindoles resulted in a mixture of spiro­[indoline-3,1′-pyrrolizines] and 7′-arylidene-substituted spirooxindoles in moderate yields. The reaction mechanism included generation of azomethine ylides, β-C–H functionalization of pyrrolidine, and sequential [3 + 2] cycloaddition. The obtained spirooxindole derivatives were investigated by in vitro evaluation against mouse colon cancer cells CT26 and human liver cancer cells HepG2 by MTT assay.

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