Histidine derivatives as tridentate chelators for the fac-[M^I(CO)₃] (Re, ^99mTc, ¹⁸⁸Re) core: Synthesis, structural characterization, radiochemistry and stability

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• 作者：Dionysia  ; Papagiannopoulou^a ;   ; ^{papagd@pharm.auth.gr} ; Charalambos  ; Tsoukalas^b ; George  ; Makris^a ;   ; ^b ; Catherine P.  ; Raptopoulou^c ; Vassilis  ; Psycharis^c ; Leondios  ; Leondiadis^b ; Ewa  ; Gniazdowska^d ; Przemyslaw  ; Ko?mi¨½ski^d ; Leon  ; Fuks^d ; Maria  ; Pelecanou^e ; Ioannis  ; Pirmettis^b ; Minas S.  ; Papadopoulos^b
• 关键词：Rhenium ; Technetium ; Tricarbonyl complexes ; Histidine derivatives
• 刊名：Inorganica Chimica Acta
• 出版年：2011
• 出版时间：30 November 2011
• 年：2011
• 卷：378
• 期：1
• 页码：333-337
• 全文大小：260 K

文摘

The development of new rhenium(I)- and technetium(I)¨Ctricarbonyl complexes can lead to potentially useful radiopharmaceuticals. In this work, the synthesis of the neutral rhenium complex fac-[Re(NSO)(CO)₃], Re-1, where NSO is the tridentate chelating agent 3-(1H-imidazol-4-yl)-2-(p-methoxy-benzylthio)propionic acid 1 was effected via reaction with (NEt₄)₂[ReBr₃(CO)₃] in the presence of NaHCO₃. Complex Re-1 crystallized from methanol/water and its structure was established by IR, ¹H and ¹³C NMR spectroscopies, ESI-MS analysis and X-ray crystallography. When the reaction took place in the absence of base, HPLC analysis revealed the presence of a second product (yield 7 % ) that was assigned by NMR and ESI analysis to be complex fac-[Re(NS)(CO)₃Br] Re-2. At the tracer level, the analogous complexes fac-[^99mTc(NSO)(CO)₃], ^99mTc-1 and fac-[¹⁸⁸Re(NSO)(CO)₃], ¹⁸⁸Re-1, were synthesized and their radiochemical stability in physiological conditions was determined. Both tracer complexes ^99mTc-1 and ¹⁸⁸Re-1 are stable in solution as well as in the presence of strongly coordinating agents like histidine or cysteine.