abstract |
(57) [Summary] (Modified) [PROBLEMS] To provide a production method for efficiently introducing a boron atom in the production of a paraboronophenylalanine derivative. A process for producing a compound of the general formula 3 from a protected aromatic amino acid derivative by reacting it with pinacol borane in the presence of a palladium catalyst and an amine. [R 1 is an amino-protecting group, R 2 is hydrogen or an amino-protecting group, R 3 is a C1-7 alkyl group or a C7-8 aralkyl group, X is iodine, bromine, chlorine or trifluoromethanesulfonyl. The oxy group or R 2 and R 3 together represent a methyl group or a carbonyl group. ] |