The utility of pyrimidine derivatives in the construction of five-membered non-azole-fused [d]pyrimidines: part III-synthetic strategies and biological applications
- 1Photochemistry Department, Chemical Industries Research Institute, National Research Centre 33 El Buhouth Street, P.O. Box 12622 Cairo Egypt +201124477409
Abstract
In recent years, considerable attention has been directed toward the construction of fused pyrimidine systems, particularly non-azolo[d]pyrimidines, due to their structural resemblance to purine analogues and their broad pharmacological potential. This review highlights the utility of pyrimidine-based precursors in the synthesis of five-membered non-azole fused [d]pyrimidine scaffolds, with special emphasis on furo[d]pyrimidine and thieno[d]pyrimidine derivatives during the last decade (2016–2026). Various synthetic methodologies are discussed, including multicomponent reactions, cyclization strategies, annulation protocols, nucleophilic substitution reactions, transition-metal-catalyzed processes, and environmentally benign approaches. In addition, the review summarizes the biological and medicinal significance of the resulting fused heterocycles, which have demonstrated promising anticancer, anti-inflammatory, antioxidant, antimicrobial and antiviral activities. Several clinically investigated and approved compounds containing thienopyrimidine frameworks are also highlighted, underscoring the pharmaceutical relevance of these privileged scaffolds. Overall, this review provides a comprehensive overview of recent advances in the synthesis and biological applications of furo[d]pyrimidine and thieno[d]pyrimidine derivatives derived from pyrimidine precursors and offers valuable insights for future developments in heterocyclic and medicinal chemistry.
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BibTeX
@article{shamroukh2026utility,
title = {{The utility of pyrimidine derivatives in the construction of five-membered non-azole-fused [d]pyrimidines: part III-synthetic strategies and biological applications}},
author = {Ahmed H. Shamroukh and Aymn E. Rashad},
journal = {RSC Advances},
year = {2026},
month = nov,
doi = {10.1039/d6ra07509f},
url = {https://doi.org/10.1039/d6ra07509f},
note = {CC BY-NC 3.0},
}
RIS
TY - JOUR
TI - The utility of pyrimidine derivatives in the construction of five-membered non-azole-fused [d]pyrimidines: part III-synthetic strategies and biological applications
AU - Ahmed H. Shamroukh
AU - Aymn E. Rashad
PY - 2026
DA - 2026/11/04
JO - RSC Advances
DO - 10.1039/d6ra07509f
UR - https://doi.org/10.1039/d6ra07509f
AB - In recent years, considerable attention has been directed toward the construction of fused pyrimidine systems, particularly non-azolo[d]pyrimidines, due to their structural resemblance to purine analogues and their broad pharmacological potential. This review highlights the utility of pyrimidine-based precursors in the synthesis of five-membered non-azole fused [d]pyrimidine scaffolds, with special emphasis on furo[d]pyrimidine and thieno[d]pyrimidine derivatives during the last decade (2016–2026). Various synthetic methodologies are discussed, including multicomponent reactions, cyclization strategies, annulation protocols, nucleophilic substitution reactions, transition-metal-catalyzed processes, and environmentally benign approaches. In addition, the review summarizes the biological and medicinal significance of the resulting fused heterocycles, which have demonstrated promising anticancer, anti-inflammatory, antioxidant, antimicrobial and antiviral activities. Several clinically investigated and approved compounds containing thienopyrimidine frameworks are also highlighted, underscoring the pharmaceutical relevance of these privileged scaffolds. Overall, this review provides a comprehensive overview of recent advances in the synthesis and biological applications of furo[d]pyrimidine and thieno[d]pyrimidine derivatives derived from pyrimidine precursors and offers valuable insights for future developments in heterocyclic and medicinal chemistry.
SN - 2046-2069
ER -