Synthesis of polyazamacrocycles with more than one type of side-

Details Synthesis of polyazamacrocycles with more than one type of side- Synthesis of polyazamacrocycles with more than one type of side-

1991-12-13

1994-05-31

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

In vivo diagnosis or in vivo testing

Magnetic imaging agent

540465, 514 79, 514185, A61K 4902, C07F 938

Patent

active

053167570

ABSTRACT:
The pH controlled selectivity of the sulfomethylation reaction is used to prepare a series of di-, tri-, tetra- and hexaazacyclomacrocycles with specified patterns of pendent side-chain chelating groups. The prepared mono and diacetic acid derivatives, together with monomethylenephosphonate and monomethylenephosphinate derivatives of tetraazacyclododecane, and triazcyclododecane and [9]aneN3, make these types of ligands easily available by a synthetic pathway that avoids the use of protective groups. The invention thus comprises a variety of compounds, methods and uses characterized by relatively high synthetic yields of polyazamacrocyclic ligands exhibiting a wide and predictable choice of metal ion binding constants water and lipid solubilities by reason of their substituent pendent groups.

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