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US 5,576,460 AGranted
Preparation of arylamines
AssigneeMassachusetts Institute of Technology
InventorsStephen L. Buchwald, Anil Guram
Life of this patent
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Abstract
A method of preparing an arylamine compound includes reacting a metal amide comprising a metal selected from the group consisting of tin, boron, zinc, magnesium, indium and silicon, with an aromatic compound comprising an activated substituent in the presence of a transition metal catalyst to form an arylamine. The method is useful in preparing mixtures of arylamines for use in screening for pharmaceutical and biological activity and in preparing poly(anilines).
Claims14
A method of preparing an arylamine compound, comprising the steps of:
- reacting an amine with an aromatic compound comprising an activated substituent at a temperature less than about 120.degree. C. in the presence of a catalyst selected from the group consisting of nickel and palladium catalyst, and a base to form an arylamine,
- wherein the aromatic compound has a formula, Ar(Z).sub.n X, and Ar is an aryl or heteroaryl moiety, X is an activated substituent selected from the group consisting of chloride, bromide, iodide, triflate, mesylate, tosylate, diazonium, and SR, where R is aryl or alkyl, and Z is selected from the group consisting of alkyl, aryl, heteroaryl, amino, carboxylic ester, carboxylic acid, acyl, hydrogen, ether, thioether, carboxamide, amide, nitro, phosphonic acid, sulphonic acid, halide, pseudohalide groups, and substituted derivatives thereof, and n is in the range of 0 to 5.
Dependencies are inferred from the claim text.