C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 17/06 (2006.01) C07K 1/13 (2006.01) C07K 16/00 (2006.01)
Patent
CA 2199387
The present invention is directed to an improved process for preparing macrocyclic chelating agents and for conjugating the macrocyclic chelating agents to biological molecules. In general, a process for preparing a chelate conjugate is disclosed which comprises purifying a polyaza chelating agent by chromatography on a silica gel column which has been acid washed prior to purification of the chelating agent, functionalizing the chelating agent with thiophosgene to form an activated isothiocyanate polyaza chelating agent which is then conjugated to a biological molecule to form a chelating agent conjugate, followed by contacting the chelating agent conjugate with a metal ion to form a chelate conjugate.
L'invention concerne un procédé amélioré de préparation d'agents chélateurs macrocycliques et de conjugaison des agents chélateurs macrocycliques avec des molécules biologiques. En général, un procédé de préparation d'un conjugué d'un chélate consiste à purifier un agent chélateur polyaza par chromatographie sur une colonne à gel de silice qui a été lavé à l'acide avant la purification de l'agent chélateur, à fonctionnaliser l'agent chélateur avec un thiophosgène pour former un agent chélateur polyaza d'isothiocyanate activé qui est ensuite conjugué à une molécule biologique pour former un conjugué de l'agent chélateur, suivi par la mise en contact du conjugué de l'agent chélateur avec un ion métal pour former un conjugué d'un chélate.
Smart & Biggar
The Dow Chemical Company
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