Abstract
Radiolabeled amino acids (AAs), their derivatives, and peptides are essential radiotracers in nuclear imaging. Despite its potential, the preparation of enantiopure radiopharmaceuticals poses several challenges, demanding a great need for rapid and stereocontrolled reactions. This chapter describes a highly stereoselective carbon-11 alkylation of Schiff bases, to obtain radiolabeled AAs and small peptides. The method uses chiral quaternary ammonium salt phase-transfer catalyst with two alkylating agents, namely, [11C]methyl iodide and [11C]benzyl iodide. This methodology allows the radiolabeling of AAs and peptides with excellent regioselectivity and enantiomeric or diastereomeric excess.
Original language | English |
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Pages (from-to) | 15-27 |
Number of pages | 13 |
Journal | Methods in molecular biology (Clifton, N.J.) |
Volume | 2729 |
DOIs | |
Publication status | Published - 2024 |
Keywords
- Amino acid
- Carbon-11
- PET imaging
- Peptide
- Radiolabeling
- Stereoselective synthesis