Metal-free iodine/NaHCO <sub>3</sub> -promoted domino synthesis of spiro-pyrimidines at room temperature with preliminary molecular docking evaluation
A metal-free protocol for the synthesis of spiro-pyrimidine derivatives has been developed via an iodine/NaHCO3-promoted domino reaction of barbituric acids with aromatic aldehydes at room temperature in 1-1.5 h. Using an EtOH-H2O (1:1) medium, the method affords diverse spiro frameworks in good to excellent yields (up to 94%) under mild and operationally simple conditions, without transition metals or harsh reagents. Mechanistic insights suggest a sequential pathway of Knoevenagel condensation, Michael addition, and iodine-assisted intramolecular cyclization. Preliminary molecular docking studies suggest possible interactions with EGFR and CYP51 targets, supporting further biological evaluation. This protocol provides a practical and sustainable route to synthetically valuable spiro-pyrimidine scaffolds.
Authors
- Samiyara Begum (ORCID: https://orcid.org/0009-0002-9470-385X)
- Fazlur Rahman
- Gaurav Rastogi
- Mohit L. Deb
- Monsur Ali
- Kazi Kawsar Ahmed
Institutions
- Institute of Organic Chemistry (PL)
- University of Science and Technology, Meghalaya (IN)
Publication Details
- Journal
- Synthetic Communications
- Published
- 2026-07-23
- DOI
- https://doi.org/10.1080/00397911.2026.2707329
- Primary Topic
- Catalytic C–H Functionalization Methods
- Type
- article
- Field-Weighted Citation Impact
- 0.00