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Heterofunctionalized phosphines as anchor groups for coupling biomolecules to the fac ‐[M(CO) 3 ] + (MRe, Tc) moiety
Author(s) -
Correia J. D. G.,
Santos I.,
Alberto R.,
Ortner K.,
Spies H.,
Drews A.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.25804401180
Subject(s) - chemistry , amide , piperazine , moiety , denticity , selectivity , chelation , stereochemistry , medicinal chemistry , phosphonate , crystallography , inorganic chemistry , organic chemistry , crystal structure , catalysis
The organometallic fac ‐[ 99m Tc(OH 2 ) 3 (CO) 3 ] + reacts with heterofunctionalized phosphines with an amide group, of the general formula HPN 2 , H 2 PNO, HPNR (R = 4‐(3‐Aminopropyl)‐1‐(methoxyphenyl)piperazine), leading to the complexes [ 99m Tc( k 3 ‐PN 2 )(CO) 3 ] (3a), [ 99m Tc( k 2 ‐H 2 PNO)X(CO) 3 ] (4a) and [ 99m Tc( k 2 ‐HPNR) X (CO) 3 ] (5a). The characterization of 3a‐5a was based on the HPLC characteristics of the corresponding Re surrogates (3–5). Under the tested experimental conditions, the more stable compounds are 4a and 5a, in which the chelate is neutral and bidentate through the phosphorus and the oxygen of the amide function. The binding affinity and selectivity of 5 for the 5HT 1A receptor were determined.