Method for producing a radiopharmaceutical

C - Chemistry – Metallurgy – 07 – C

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C07C 227/12 (2006.01) C07C 229/36 (2006.01)

Patent

CA 2757402

The invention relates to a method for producing a radiopharmaceutical. In said method, steps (A), (B), and (C) are performed. In a step (A), an H-Li exchange is made by adding an alkyllithium to an isocyanide, wherein the .alpha.-H atom of the isocyanide is replaced with an Li atom. In a step (B), 11CO2 is added and bonded to the .alpha.-C atom of the isocyanide. By means of a two-stage hydrolysis in step (C), the Li atom is replaced with an H atom and an amino group is formed from the isocyanide group, for example, by adding NH4Cl and HI. According to the invention, the reaction is continuously performed in particular in a microfluidic structure so that reaction times of less than 300 seconds can be achieved for the partial steps (A, B). Because the produced radiopharmaceutical has only a low half-life, the short production time has a positive effect on the yield of radioactive pharmaceutical.

L'invention concerne un procédé de production d'un composé radiopharmaceutique, procédé comprenant les étapes (A), (B) et (C). Dans une étape (A), on effectue un échange H-Li, par addition d'un alkyl-lithium à un isocyanure, l'atome H-a de l'isocyanure étant remplacé par un atome Li. Dans une étape (B), le 11CO2 est ajouté et est lié à l'atome C-a de l'isocyanure. Par hydrolyse en deux stades dans l'étape (C), par addition, par exemple de NH4Cl et de HI, l'atome Li est remplacé par un atome H, et il se forme, à partir du groupe isocyanure, un groupe amino. L'invention est caractérisée en ce que la réaction s'effectue en continu, en particulier dans une structure microfluide, de manière à avoir, pour les étapes partielles (A, B) des temps de réaction inférieurs à 300 secondes. Etant donné que le composé radiopharmaceutique produit n'a qu'une faible période, le temps de production court se répercute positivement sur le rendement en composé pharmaceutique radioactif.

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