N-4 Alkyl Cytosine Derivatives Synthesis: A New Approach

Autor: Mauro De Nisco, Antonio Di Maio, Michele Manfra, Carmine Ostacolo, Alessia Bertamino, Pietro Campiglia, Isabel M. Gomez-Monterrey, Silvana Pedatella
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Reactions, Vol 3, Iss 1, Pp 192-202 (2022)
Druh dokumentu: article
ISSN: 2624-781X
DOI: 10.3390/reactions3010014
Popis: The selective N-4 alkylation of cytosine plays a critical role in the synthesis of biologically active molecules. This work focuses on the development of practical reaction conditions toward a regioselective synthesis of N-4-alkyl cytosine derivatives. The sequence includes a direct and selective sulfonylation at the N-1 site of the cytosine, followed by the alkylation of the amino site using KHMDS in CH2Cl2/THF mixture, providing a fast and efficient approach consistent with pyrimidine-based drug design.
Databáze: Directory of Open Access Journals