Method for rapid fluoromethylation and method for preparation of PET tracer using the same

摘要

Provided are: a method for rapid fluoromethylation, by which a fluoromethyl group can be easily bonded to an aromatic-ring carbon of an aromatic compound with little generation of by-products; and a process for preparation of a PET tracer using the same. The method is characterized by cross-coupling an organoboron compound in which an aromatic ring is bonded to a boron atom with FCX2Br (wherein X is ordinary hydrogen or heavy hydrogen) in a solvent obtained by adding water to an aprotic polar solvent, in the presence of a palladium complex, a phosphine ligand, and a base.

主权项

1. A method for rapid fluoromethylation, wherein an organoboron compound in which an aromatic ring, an alkenyl group or an alkynyl group is bonded to a boron atom is cross-coupled with FCX2Br (wherein X is ordinary hydrogen or heavy hydrogen) in the presence of a palladium complex, a phosphine ligand, and a base, in a solvent obtained by mixing water and N,N′-dimethylpropyleneurea, the reaction being performed at a temperature of from 90° C. to 120° C., and wherein the ratio of the volume of water to the volume of N,N′-dimethylpropyleneurea is in the range 0.05 to 0.15 inclusive.