Method for manufacturing arylamines

摘要

Preparation of aryl- or heteroaryl amine or aryl- or heteroaryl amide comprises cross coupling of primary or secondary amine or amide with substituted aryl- or heteroaryl compound, in the presence of a Bronsted base and a catalyst or pre-catalyst; where the catalyst is a transition metal, complex, salt or compound of transition metal such as nickel or palladium, or at least a ligand such as a bidentate bis(phosphino)alkanediyl compound, in a solvent or solvent mixture. Preparation of aryl- or heteroaryl amine or aryl- or heteroaryl amide comprises cross coupling of primary or secondary amine or amide with substituted aryl- or heteroaryl compound, in the presence of a Bronsted base and a catalyst or pre-catalyst; where the catalyst is a transition metal, complex, salt or compound of transition metal such as nickel or palladium, or at least a ligand such as a bidentate bis(phosphino)alkanediyl compound of formula (Ar1>-P(Ar2>)-L-P(Ar3>)(Ar4>)), in a solvent or solvent mixture. Ar1>-Ar4>aryl- or heteroaryl-substituent such as phenyl, naphthyl, pyridyl or biphenyl, where hydrogen is optionally substituted by lower-alkyl, halo, sulfonic acid group, carboxylic acid group, lower alkyloxy substituent, or H, 1-2C alkyl, linear, branched or cyclic 3-8C alkyl, which is optionally substituted with Cl, Br, I, OH, NH2, NO2, CN, COOH, lower-alkyl-amine, lower alkyl-diamine, lower-alkyl-oxy, lower-alkyl-oxycarbonyl or lower-alkyl-carbonyloxy, where the lower alkyl is 1-4C alkyl; and L : 1-20C (preferably 1-4C) alkanediyl bond, preferably ethane-1,2-diyl, propane-1,3-diyl, butane-1,4-diyl or 2,2-dimethylpropane-1,3-diyl.