SYNTHESIS OF POLYAZACYCLOALKANES

von Khadija Nabih

52 Seiten, Taschenbuch

Kurzbeschreibung des Verlags

This article presents organic synthesis work aimed at functionalizing tetraazamacrocycles, notably Cyclam and Cyclen, for use as chelating agents in medical imaging (MRI) and radiopharmaceuticals. These polyazotated cyclic ligands, such as DOTA used in Dotarem®, are crucial for stably and selectively complexing metals (Gd³¿, Bi³¿). The synthesis strategy relies on a sequence of protection, functionalization, and deprotection. A key step is the protection of three of the four amines in the macrocycle with a phosphoryl group, using tris(dimethylamino)phosphine. This selective protection leaves a single free amine available for subsequent modification. This amine is then functionalized with electrophilic derivatives (R-X), resulting in mono-N-substituted macrocycles. Bis-functionalization is then carried out by alkylation with ethyl bromoacetate, followed by hydrolysis to obtain carboxylic acid groups. The experimental section describes in detail the protocols for synthesis, oxidation, and hydrolysis, as well as the purification of the compounds.

• Themen: Mathematik und Naturwissenschaften Chemie Organische Chemie
• ISBN: 9786630116960
• Sprache: Englisch
• Erscheinungsdatum: 21.09.2026
• Größe: 220 x 150 mm
• Verlag: Our Knowledge Publishing