| 摘要 |
A method for preparing a beta-boronated alpha,beta-unsaturated carbonyl compound is provided to beta-boronate the alpha,beta-unsaturated carbonyl compound efficiently, thereby being applied to prepare boron added compounds at various beta positions and being useful for forming a product in an aspect of BNCT(boron neutron capture therapy). A method for preparing a compound where a boron is added at a beta position comprises a step of reacting an alpha,beta-unsaturated carbonyl compound represented by the formula(1) with a diboronate compound at a temperature of 25-50 deg.C in a solvent such as dimethyl formamide, toluene and tetrahydrofuran in the presence of a Cu catalyst such as CuCl/NaOt-Bu, Cu(OAc) and CuOtBu, a base, and a phosphine ligand or a C1-6 primary to tertiary alcohol. In the formula(1), R is H, C1-10 alkyl, phenyl, substituted or unsubstituted C6-14 aromatic, or C6-12 hetero aromatic including at least one N and O; R' is H or C1-10 alkyl; and EWG is ketone or ester. Further, a ligand selected from Xantphos, DPEphos, Tributylphosphine and Tricyclohexylphosphine is additionally added when reacting.
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