A convenient synthesis of novel bifunctional prochelators for coupling to bioactive peptides for radiometal labelling.
New DOTA-based bifunctional prochelators, e.g., 1-(1-carboxy-3-carbotertbutoxypropyl)-4,7,10-(carbotertbutoxyme thyl)-1,4,7,10-tetraazacyclodode-cane (DOTAGA(tBu)4), (6d) for a broad application in the modification of biomolecules with metal ions were prepared. The five-step synthesis of 6d has an overall yield of about 20%. The coupling of 6d to a bioactive peptide on solid-phase was exemplified with use of a CCK-B (cholecystokinin) analogue.
Eisenwiener
K P
KP
University Hospital, Basel, Switzerland.
Powell
P
P
Mäcke
H R
HR
D002614:Chelating Agents / Q000138:chemical synthesis*; D002766:Cholecystokinin / Q000138:chemical synthesis; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000138:chemical synthesis; D009942:Organometallic Compounds / Q000138:chemical synthesis; D011355:Prodrugs / Q000138:chemical synthesis*; D011868:Radioisotopes / Q000737:chemistry
D002614:Chelating Agents; D009842:Oligopeptides; D009942:Organometallic Compounds; D011355:Prodrugs; D011868:Radioisotopes; D002766:Cholecystokinin