申请人:Oxford University Innovation Limited
公开号:US20170137341A1
公开(公告)日:2017-05-18
The present invention relates to a process for producing an organic compound comprising an
18
F atom. The compounds comprising an
18
F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp
2
hybridised carbon atom, with (i)
18
F— and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp
2
hybridised carbon atom, in a process for producing an organic compound comprising an
18
F atom, which process comprises treating the organoboron compound with (i)
18
F— and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PG
A
is independently H or an alcohol protecting group; PG
B
is H or a carboxylic acid protecting group; each PG
C
is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4.