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US 9,315,474 B2Granted
Process for the preparation of macrocyclic polyazacarboxylate ligands and chelates
AssigneeLiebel-Flarsheim Company
InventorsDennis A. Moore, Raghavan Rajagopalan
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Abstract
The present disclosure relates generally to a process for the synthesis of 1,4,7,10 -tetraazacyclododecane ligands, chelates, and derivatives thereof. In particular, the present disclosure is directed to a process for the synthesis of 1,4,7,10-tetraaza-1,4,7,10-tetrakis(carboxymethyl)cyclododecane (DOTA) ligands, corresponding DOTA-metal chelates, and various derivatives thereof.
Claims20
A process for the preparation of a macrocyclic tetramer compound of Formula (II), the process comprising:
- (i) forming a reaction mixture comprising a stoichiometric amount of (a) an aziridine of Formula (I), (b) a Brønsted acid, a Lewis acid, or a combination of a Brønsted acid and a Lewis acid, and (c) a solvent;
- and,
- (ii) reacting the contents of the reaction mixture to form the compound of Formula (II) by cyclotetramerization of the aziridine of Formula (I), according to the following reaction:
- wherein:
- each R1 is independently selected from the group consisting of C1-10 hydrocarbyl.
2 more elements
Dependencies are inferred from the claim text.