Lithiation of Functionalized Fluoroquinolines: Synthesis of Dihalo-2-phenylquinoline-4-carboxamides and in Vitro Evaluation as NK-3 Receptor Ligands for Medical Imaging Studies

Autor: Louisa Barré, Sylvie Tymciu, Cécile Perrio, Florence Mongin, Marie‐Claire Lasne, Idriss Bennacef, Martine Dhilly, Guy Quéguiner
Rok vydání: 2004
Předmět:
Zdroj: The Journal of Organic Chemistry. 69:2622-2625
ISSN: 1520-6904
0022-3263
DOI: 10.1021/jo0358426
Popis: Fluoroiodo-2-phenylquinoline-4-carboxamides, analogues of NK-3 antagonist SB 223412, were synthesized and evaluated as NK-3 ligands with the aim of developing radioligands suitable for both Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) studies. The key step utilizes metalation directed by the fluorine atom for iodination of the quinoline ring.
Databáze: OpenAIRE