Method of synthesizing compounds having a...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/14 (2006.01) A61K 51/00 (2006.01) C07B 59/00 (2006.01)

Patent

CA 2555305

Provided are methods for synthesizing radiotracers, including no carrier added (n.c.a.) tracers suitable as PET scan tracers that contain a 18F-P bond. The radiolabeled products may be synthesized from precursors including phosphorus(V) and/or phosphorus (III) atoms bound to a suitable leaving group or group(s). For example, precursors incorporating a nitrophenoxy leaving group bound to a phosphorus(V) atom tend to exhibit an acceptable combination of stability and reactivity and also tend to allow the precursor compound(s) to be separated more easily from the 18F labeled products. The methods disclosed herein for producing radiolabeled compounds incorporating a P-18F chemistry may particularly useful radiolabeling oligonucleotides, phospholipids, phosphorilated proteins, sugars and steroids for use as PET radiotracer compounds for medical imaging applications.

L'invention concerne des méthodes de synthèse de radiotraceurs, notamment des traceurs sans support ajouté (n.c.a.) appropriés en tant que traceurs de balayage PET, contenant une liaison ?18¿F-P. Les produits radiomarqués peuvent être synthétisés à partir de précurseurs, notamment des atomes de phosphore (V) et/ou de phosphore (III) reliés à un ou à plusieurs groupes partants. Par exemple, des précurseurs comprenant un groupe partant nitrophénoxy relié à un atome de phosphore (V) tend à présenter une combinaison acceptable de stabilité et de réactivité, et de tels précurseurs permettent également de séparer plus facilement le ou les composés précurseurs des produits marqués ?18¿F. Les méthodes de production de composés radiomarqués intégrant une chimie P-?18¿F peuvent s'avérer particulièrement utiles pour le radiomarquage d'oligonucléotides, de phospholipides, de protéines phosphorylées, de sucres et de stéroïdes à utiliser en tant que composés radiotraceurs PET pour des applications d'imagerie médicale.

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