Patent ID: 7196219

Claim:
A process for preparing an anilineboronic acid derivative of the formula I comprising the steps of: step 1: converting an aniline (II) to a diprotected aniline (III) by introducing two protecting groups PG, step 2: metalating the diprotected aniline (III) with a metalating agent and simultaneously or subsequently reacting with a boronic ester B(OR 1,2,3 ) 3 (IV) to a protected anilineboronic ester of the formula (V), and step 3: detaching the protecting groups PG, to form the anilineboronic ester of the formula (I) Step 1: Protection of the aniline by dibenzylation Step 2: Metalation of the protected aniline, conversion to boronic acid derivative Step 3: Detachment of the protecting group where R is H, F, Cl, Br, I, a branched or unbranched, substituted or unsubstituted C 1 –C 20 —, a substituted or unsubstituted C 6 –C 12 -aryl or -aryloxy radical, a heteroaryl radical, a heteroaryloxy radical, a substituted or unsubstituted C 3 –C 8 -cycloalkyl radical, a dialkyl group, a diarylamino group, an alkyl group, an arylthio group, an ester group or acetal group; X is H, Cl, Br, I or F; R 1 , R 2 , R 3 are each independently H, a branched or unbranched, substituted or unsubstituted C 1 –C 20 -alkyl group, and two R 1-3 radicals together may optionally form a ring, or are each further B(OR 1,2,3 ) 3 radicals.