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Synthesis of iodinated and radioiodinated ( E )‐N‐(3‐iodoprop‐2‐enyl)‐2β‐carbomethoxy‐3β‐(3′,4′‐dichlorophenyl) nortropane (β‐CDIT): a ligand for the dopamine transporter
Author(s) -
Emond P.,
Boazi M,
Duchêne A.,
Chalon S.,
Besnard J. C.,
Guilloteau D.,
Frangin Y.
Publication year - 1997
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/(sici)1099-1344(199709)39:9<757::aid-jlcr24>3.0.co;2-j
Subject(s) - chemistry , dopamine transporter , in vivo , ligand (biochemistry) , tropane , iodine 123 , stereochemistry , transporter , dopamine , derivative (finance) , medicinal chemistry , biochemistry , receptor , medicine , financial economics , economics , microbiology and biotechnology , biology , gene
The synthesis of ( E )‐N‐(3‐iodoprop‐2‐enyl)‐2β‐carbomethoxy‐3β‐(3′,4′‐dichlorophenyl) nortropane (β‐CDIT) and its radioiodinated analogues is described. Three different synthetic methods are reported for the preparation of ( E )‐N‐[3‐(tributylstannyl)‐2‐enyl]‐2β‐carbomethoxy‐3β‐(3′,4′‐dichlorophenyl) nortropane, which was iododestannylated for the preparation of the corresponding iodinated derivative. We also report the radiolabelling of β‐CDIT with 125 I or 123 I that could be used for in vitro and in vivo exploration of the dopamine transporter. © 1997 John Wiley & Sons, Ltd.