Ｌ−３，４−ジヒドロキシ−６−［１８Ｆ］フルオロ−フェニルアラニン及び２−［１８Ｆ］フルオロ−Ｌ−チロシン及びそれらのα−メチル化誘導体の前駆体の製造方法、前駆体、この前駆体からのＬ−３，４−ジヒドロキシ−６−［１８Ｆ］フルオロ−フェニルアラニン及び２−［１８Ｆ］フルオロ−Ｌ−チロシン及びそれらのα−メチル化誘導体の製造方法

摘要

Substituted benzaldehyde compounds (I), are new. Substituted benzaldehyde compounds of formula (I), is new. X : H or CH 3; R 5>nucleophilic leaving group e.g. B, F, Br, Cl, NO 2or -N(R) 3 +>; R : alkyl e.g. CH 3or C 2H 5; R 2>benzyl or methyl; and R 4>(S)-1-(tert-butoxycarbonyl)-2-tert-butyl-3-methyl-4-imidazolidinone, (S)-1-(benzoylcarbonyl)-2-tert-butyl-3-methyl-4-imidazolidinone, (S)-tert-butyl-2-tert-butyl-4-methoxy-2,5-dihydroimidazol-1-carboxylate, (2S,5R)-tert-butyl-2-tert-butyl-3,5-dimethyl-4-oxoimidazolidin-1-carboxylate, (S)-1-(benzoylcarbonyl)-2-tert-butyl-3,5-dimethyl-4-imidazolidinone or (S)-tert-butyl-2-tert-butyl-5-methyl-4-methoxy-2-hydroimidazol-1-carboxylate. Independent claims are included for: (1) the preparation of (I); and (2) preparing L-3,4-dihydroxy-6-[18F]fluorophenylalanine compound of formula (II) and 2-[18F]fluoro-L-tyrosine compound of formula (III), comprising [18F]-fluorinating (I), separating the fluorinated compound in which the fluorinated compound is oxidized to give (II) or decarbonylated to give (III), and hydrolyzing and separating the respective products. [Image] [Image].