Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Regular Article
P(III)-Mediated Formal Reductive N–H Bond Insertion Reaction of Hydrazones to α-Keto Esters
Norihiko TakedaTomoki MiyashitaNaoya HirokawaMotohiro YasuiMasafumi Ueda
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2024 年 72 巻 4 号 p. 413-420

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A diazo-, metal-, and base-free multi-substituted hydrazone synthesis via a formal reductive N–H bond insertion reactions of hydrazones to α-keto esters has been developed. The protocol features a broad substrate scope and good functional group tolerance, providing N–H bond insertion products in moderate to excellent yields. Moreover, P(III)-mediated N–H functionalization of pharmaceutical containing hydrazone moiety was also successfully achieved.

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© 2024 Author(s)
Published by The Pharmaceutical Society of Japan

This article is licensed under a Creative Commons [Attribution-NonCommercial 4.0 International] license.
https://creativecommons.org/licenses/by-nc/4.0/
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