Simplified one-pot synthesis of [¹⁸F]SFB for radiolabeling

摘要

A non-aqueous single pot synthesis of [18F]SFB is set forth. The [18F]SFB produced with this method is then used, for example, to label a peptide or an engineered antibody fragment (diabody) targeting human epidermal growth factor receptor 2 (HER2) as representative examples of labeled compounds for use as an injectable composition to locate abnormal tissue, specifically tumors within an animal or human using a PET scan.

主权项

1. An anhydrous process for preparing 18F labeled compounds comprising
a labeling step comprising, reacting an alkyl or aryl 4-trimethylammoniumbenzoate triflate with a dried potassium-Kryptofix-2.2.2 complex salt of [18F]fluoride, or a cesium salt of [18F]fluoride, in dimethylsulfoxide (DMSO), to provide a corresponding alkyl or aryl 4-[18F]fluorobenzoate solution, a deprotecting step comprising dissolving the alkyl or aryl 4-[18F]fluorobenzoate in a basic anhydrous/aprotic solvent to provide a reaction mixture containing 4-[18F]fluorobenzoate salt, and a coupling step comprising adding a solution of an activating agent to the reaction mixture contained 4-[18F]fluorobenzoate to provide an activated ester wherein the process include reacting the activated ester with a primary amine containing compound to provide a radiolabeled compound.