4.7 Article

Palladium-Catalyzed Ring-Closing Reaction for the Synthesis of Saturated N-Heterocycles with Aminodienes and N,O-Acetals

期刊

JOURNAL OF ORGANIC CHEMISTRY
卷 86, 期 11, 页码 7849-7863

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.1c00752

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  1. National Natural Science Foundation of China [21925111, 21790333]

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This efficient palladium-catalyzed ring-closing reaction allows for the synthesis of saturated N-heterocycles with diverse structural backbones, using volatile MeOH as the sole byproduct. This method provides a rapid and practical access to a broad range of useful building blocks in natural product synthesis and drug discovery.
An efficient palladium-catalyzed ring-closing reaction of aminodienes with N,O-acetals for the synthesis of saturated N-heterocycles is described. The reaction is consistently operated at room temperature and tolerates a wide range of functional groups with volatile MeOH as the sole byproduct. This method provides rapid and practical access to a broad range of saturated N-heterocycles with diverse structural backbones that are useful building blocks in natural product synthesis and drug discovery.

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