Structurally diverse pyrroles were synthesized via direct coupling of α, β-unsaturated aldehydes and phenacyl azides at ambient temperature without using any strong base or transition metal catalyst. The reaction offers great compatibility in prod...
Artikel
Visible‐Light‐Driven Three‐Component Reaction of Unactivated Alkenes Enables Access to Monofluoro γ‐Amino Acids
Von Wiley-VCH zur Verfügung gestellt
A strategy for the synthesis of diverse protected α-monofluoro-γ-amino acid derivatives has been developed. This reaction conveniently and efficiently provides monofluoroamino acid ethyl ester-quinoxaline-2(1H)-one derivatives under mild conditions. Using removable amide carbonyl alkenes provides an efficient strategy for the preparation of various α-monofluoro-γ-amino acid derivatives. This strategy has the advantages of metal-free, mild conditions, simple operation, and environmentally friendly energy sources.
Abstract
A strategy for the synthesis of diverse protected α-monofluoro-γ-amino acid derivatives has been developed. This reaction assembles a simple enamide, quinoxalin-2(1H)-one, and diethyl 2-bromo-2-fluoromalonate through a three-component reaction driven by visible light. The advantages of this protocol include the simplicity of its operation, mild conditions, high functional group tolerance, and applicability to a wide variety of substrates. The synthesis of this fluorine-containing amino acid derivative has significant value for potential applications in medicinal chemistry and chemical biology.
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