Abstract: The invention relates to a method for preparation of aminoaryl- or aminoheteroarylboronic acids and esters and salts thereof in which an optionally substituted aminoaryl or aminoheteroaryl compound is protected at its nitrogen site via condensation with a carbonyl compound, subsequently metalated and converted with a suitable boron compound.

Abstract: A process for preparing anilineboronic acid derivative of the formula I, by converting an aniline to a diprotected aniline by introducing two protecting groups, metalating the diprotected aniline with a metalating agent and simultaneously or subsequently reacting with a boronic ester B(OR1,2,3)3 to form a protected anilineboronic ester, which is converted, by detaching the protecting groups, to the anilineboronic esters of the formula (I).

Abstract: The invention relates to a method for the production of substituted aromatic compounds by producing lithium arylene and by reacting it with suitable electrophiles. The method comprises the following steps (step 1); an aryl lithium compound ( auxiliary base”) is initially produced by reacting a halogen aromatic compound with lithium metal; said compound is subsequently (step 2) reacted for deprotonation of the aromatic substrate in order to form the corresponding lithium aromatic compound which is subsequently (step 3) reacted with a corresponding electrophile to form the desired substituted aromatic compound, see page 2 of the description.

Abstract: The invention relates to a method for binding heteroatom-carbon bonds. According to said method, a lithium compound (II) is first generated by reacting aliphatic or aromatic halogen compounds (I) with lithium metal, said compound is then used for the deprotonation of the compounds (III) or (V). The lithium salts of formulas (IV) or (VI) obtained by said deprotonation are subsequently reacted with suitable carbon electrophiles (equation I), said process binding the heteroatom-carbon bond and forming the products (VIII) or (VIII), (equation I).

Abstract: A process for preparing anilineboronic acid derivatives of the formula I, by converting an aniline (II) to a diprotected aniline (III) by introducing two protecting groups PG, metalating (III) and simultaneously or subsequently reacting with a boronic ester B(OR1,2,3)3 (IV) to a protected anilineboronic ester of the formula (V), which is converted, by detaching the protecting groups PG, to the anilineboronic esters 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 for example, H, F, Cl, Br, I, a, C1-C20—,alkyl or -alkoxy radical, a C6-C12-aryl or -aryloxy radical, a heteroaryl or heteroaryloxy radical, a C3-C8-cycloalkyl radical; X is H, Cl, Br, I or F; R1, R2, R3 are each independently H, a C1-C20-alkyl group, and two R1-3 radicals together may optionally form a ring, or are each further B(OR)3 radicals.