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Updated: Jul 23, 2025

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
N-Alkyl Carbamoylimidazoles as Versatile Synthons for the Synthesis of Urea-Based PSMA Inhibitors
Narendar Reddy Gade1, Jatinder Kaur1, Atul Bhardwaj1
1Department of Oncology, University of Alberta, Edmonton, Alberta T6G 1Z2, Canada.
Abstract:
We describe N-alkyl carbamoylimidazoles as readily available and highly versatile synthons for synthesizing urea-based prostate-specific membrane antigen (PSMA) inhibitors. Urea formation proceeded in high yields (>80%) at room temperature under aqueous conditions. All novel compounds were tested for their PSMA inhibitory potency in a cell-based radiometric binding assay. Compound 17 was identified as a novel high-affinity PSMA inhibitor (IC50 = 0.013 μM) suitable for developing an 18F-labeled radioligand for PET imaging of PSMA in prostate cancer.
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