公开(公告)号：EP4249058A1

公开(公告)日：2023-09-27

申请号：EP21894737.2

申请日：2021-11-18

申请人： National Center for Geriatrics and Gerontology

发明人： SUZUKI Masaaki ,  ITO Kengo ,  KIMURA Yasuyuki ,  OGATA Aya ,  IKENUMA Hiroshi ,  KIMURA Tetsuya ,  KIMURA Nobuyuki ,  KOYAMA Hiroko ,  ISHII Hideki ,  CHO Meiei ,  KAWAMURA Kazunori ,  MINAMIMOTO Takafumi ,  NAGAI Yuji ,  KATSUKI Hiroshi

IPC分类号： A61P25/00 ,  C07C51/09 ,  C07C57/03 ,  C07C403/20 ,  C07B61/00 ,  C07C67/343 ,  A61K51/04 ,  C07C69/587 ,  A61K31/202

摘要： [Object] Provided are a 11 C-labeled acyclic retinoid that can be synthesized in a short time with a high yield and can be suitably used for PET for elucidating intracerebral kinetics, a PET probe using it, and methods for producing them.
[Solution] The 11 C-labeled acyclic retinoid of the present invention is characterized by being represented by the following chemical formula (a). This compound can be produced by a coupling step of cross-coupling a methyl iodide labelled with 11 C and the following organotin compound (b) (provided that in the formula, R 1 and R 2 represent alkyl groups which may have a branch) in an aprotic solvent in the presence of a palladium complex, a phosphine ligand, and a cuprous halide.