Palladium-Catalyzed Cascade Reaction Involving Cyclopropenones Enables Construction of Heterocycle-Containing
Ting-You Yang1,2, Jing Cui1,2, Ming-Yu Yang1,2
1Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals, Zunyi Medical University, Zunyi 563000, China.
Abstract:
A novel palladium-catalyzed cascade reaction process for the diverse synthesis of heterocycle-containing γ-alkylidenebutenolide frameworks has been developed. Using this protocol, γ-alkylidenebutenolide and δ-heterocycle units can be constructed simultaneously through one-pot multiple C-C/C-O bond formation of different iodoaryl-substituted alkenes with cyclopropenones, leading to nine types of heterocycle-containing γ-alkylidenebutenolides in generally acceptable yields. The advantage of this work is also featured by its gram-scale preparation, further diverse transformations, and good in vitro antitumor activities of the highly valuable and modifiable synthetic products.
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