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Synthesis 2023; 55(03): 457-464
DOI: 10.1055/a-1942-7191
DOI: 10.1055/a-1942-7191
paper
Na2CO3-Mediated [3+3] Annulation Reaction of Substituted Benzamidines with 2-Benzylidenemalononitriles: Access to Substituted Pyrimidine-4,6-diamines
This research was financially supported by the Priority Academic Program Development of Jiangsu Higher Education Institutions.
Abstract
An efficient protocol for the synthesis of 2-aryl-5-benzylpyrimidine-4,6-diamines from readily available substituted 2-benzylidenemalononitriles and substituted benzamidines was developed. This practical protocol provides high value pyrimidine-4,6-diamines in moderate to good yields under simple reaction conditions. This approach also enables some modifications of structurally complex bioactive molecules and exhibits potential applications in medicinal chemistry.
Key words
4,6-diaminopyrimidines - 2-benzylidenemalononitriles - benzamidines - annulation reaction - N-heterocyclesSupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/a-1942-7191.
- Supporting Information
Publication History
Received: 07 August 2022
Accepted after revision: 14 September 2022
Accepted Manuscript online:
14 September 2022
Article published online:
24 October 2022
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