Patent ID: 7196219
Filing Date: 2007-03-27
Classification: C07F,Y02P

Abstract:
1. 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 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 X is H, Cl, Br, I or F; R