Electrochemically Promoted Amination of Pyrido[2,3‐d]pyrimidin‐7‐ones: Efficient Synthesis of Palbociclib Derivatives

The pyrido[2,3‐ d ]‐pyrimidin‐7‐one template is a crucial molecular fragment in antineoplastic drug palbociclib. Considering the importance of pyrido[2,3‐ d ]‐pyrimidin‐7‐one template, herein, a simple and environmentally friendly electrocatalytic amination of pyrido[2,3‐ d ]pyrimidin‐7‐ones is reported with N,N ‐dialkyl formamides as the amine source and NaBr as the electrolyte. This straightforward and operationally simple protocol opens a green and efficient strategy for the synthesis of palbociclib derivatives in moderate to good yields.

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Publication Details

Journal
European Journal of Organic Chemistry
Published
2025-04-26
DOI
https://doi.org/10.1002/ejoc.202500259
Primary Topic
Synthesis and Biological Evaluation
Type
article
Field-Weighted Citation Impact
0.00

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article

Electrochemically Promoted Amination of Pyrido[2,3‐d]pyrimidin‐7‐ones: Efficient Synthesis of Palbociclib Derivatives

Qing Zhu, Zhang Li-xi, Chao Shen, Dong Wang et al.
European Journal of Organic Chemistry
Synthesis and Biological Evaluation
article

Electrochemically Promoted Amination of Pyrido[2,3‐d]pyrimidin‐7‐ones: Efficient Synthesis of Palbociclib Derivatives

Qing Zhu, Zhang Li-xi, Chao Shen, Dong Wang, Jiabin Shen, Pengfei Zhang
article en

Abstract

The pyrido[2,3‐ d ]‐pyrimidin‐7‐one template is a crucial molecular fragment in antineoplastic drug palbociclib. Considering the importance of pyrido[2,3‐ d ]‐pyrimidin‐7‐one template, herein, a simple and environmentally friendly electrocatalytic amination of pyrido[2,3‐ d ]pyrimidin‐7‐ones is reported with N,N ‐dialkyl formamides as the amine source and NaBr as the electrolyte. This straightforward and operationally simple protocol opens a green and efficient strategy for the synthesis of palbociclib derivatives in moderate to good yields.

European Journal of Organic ChemistryVol. 28(24)
Hangzhou Normal University (CN), Zhejiang Shuren University (CN), Zhejiang University of Technology (CN)
National Natural Science Foundation of China, Natural Science Foundation of Zhejiang Province
Openalex Percentile: Top 93%
Synthesis and Biological Evaluation
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