专利号:WO-2025108921-A1 优先权日:2023-11-22 标 题 :Synthesis of radiopharmaceutical agents 发明人:AUZELOUX PHILIPPE; LEVESQUE SOPHIE; GALMIER MARIE-JOSÈPHE; CHEZAL JEAN-MICHEL 权利人:INST NAT SANTE RECH MED; UNIV CLERMONT AUVERGNE; CENTRE LUTTE CONTRE LE CANCER 摘要:Synthesis of radiopharmaceutical agents It is disclosed a method to synthesize a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I), (I) said process comprising contacting a trialkylstannane precursor of formula (II), or a pharmaceutically acceptable salt thereof: Formula (II), (II) with an alkali metal salt of a radionuclide selected from the group consisting of 123I, 124I, 125I, 131I, 211At, in appropriate acidic conditions and in presence of a peroxide ROOH in an 10 appropriate concentration. Said method is particularly suited for synthesizing [131I]N-(2- diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide, providing a notable reduction in the quantity of side products, allowing a much purer finished product, while making use of reagents which are adapted to the constraints which need to be met when developing a product for clinical use and, more in particular, to the constraints to be met in order to 15 adapt the process for being fully automated.
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