Iron‐Mediated Electrophilic Amination of Organozinc Halides using Organic Azides

阅读量:

13

作者:

S GraßlJ SingerP Knochel

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摘要:

A wide range of alkyl aryland heteroarylzinc halides have been aminated with highly functionalized alkyl, aryl and heterocyclic azides. The reaction proceeds smoothly at 50 °C within 1 h in the presence of FeCl3 (0.5 equiv) to furnish the corresponding secondary amines in good yields. This method was extended to peptidic azides, providing the arylated substrates under full retention configuration. To demonstrate the utility of this reaction, we prepared two amine derivatives of pharmaceutical relevance using this iron﹎ediated electrophilic amination as the key step.

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DOI:

10.1002/anie.201911704

年份:

2020

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