Synthesis and Applications of 4-Chloro-2-(trichloromethyl)pyrimidines

A Synthesis of 4-Chloro-2-(trichloromethyl)pyrimidines and Their Study in Nucleophilic Substitution: M. L. Trujillo-Lagunas, I. Medina-Mercado, I. Zaragoza-Galicia, H. F. Olivo, M. Romero-Ortega
Synthesis 2019, DOI: 10.1055/s-0037-1610270


The pyrimidine nucleus is present in a number of important and bioactive organic compounds, thus the interest in densely functionalized pyrimidine building blocks to be used in synthesis. Recently, a publication from the group of Professor Moisés Romero-Ortega from the Universidad Autónoma del Estado de México (Toluca, Mexico) described novel chemistry aimed at preparing and using 2-trichloromethyl-4-chloropyrimidines for the synthesis of a wide range of substituted pyrimidines.

Professor Romero-Ortega said: “2-Trichloromethyl-4-chloropyrimidines, easily synthesized by an acylation/cyclization-chlorination process, served as valuable intermediates in substitution reactions for the synthesis of a variety of pyrimidine derivatives. The formation of these products could be explained by the softness and hardness principle of the nucleophile involved.”
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