Process for the coupling of benzylamines and halogenated aromates

摘要

Preparing optionally substituted arylated benzylamines comprises reacting optionally substituted benzylamines with optionally substituted aryl halides. The reaction is effected in the presence of palladium complex bearing bisaryldialkylphosphine compound(s) as ligand, in the presence of mixtures of organic solvents comprising optionally substituted aromatic hydrocarbons and polar solvent(s) and in the presence of alkali metal or alkaline earth metal-containing base(s). Preparing optionally substituted arylated benzylamines of formula (I) comprises reacting optionally substituted benzylamines of formula (II) with optionally substituted aryl halides of formula (III). The reaction is effected in the presence of palladium complex bearing bisaryldialkylphosphine compound(s) of formula (IV) as ligand, in the presence of mixtures of organic solvents comprising optionally substituted aromatic hydrocarbons and polar solvent(s) and in the presence of alkali metal or alkaline earth metal-containing base(s). R 1>-R 10>H, 1-12C alkyl or (fluoro)alkoxy, 4-18C aryl, 5-19C arylalkyl, nitrile, ester, amide, ketone, aldehyde, OH, COOH, or F; X : Cl, Br or I; R 11>, R 12>1-12C alkyl or 5-19C arylalkyl; R 13>, R 14>H or 1-6C alkyl, dialkylamino or alkoxy; R 15>H, 1-12C (fluoro)alkyl or (fluoro)alkoxy, F, 4-18C aryl, or 5-19C arylalkyl, where the arrows indicate the possible bonding sites to the particular aryl radical; and n, m : 0-3. [Image] [Image].