US 8,785,651 B2 · Method for manufacturing a boronic acid ester compound

Abstract

The present invention relates to a method for manufacturing a boronic acid ester compound, characterized by reacting an aryl halide compound and a diboron ester compound in the presence of a nitrogen-containing organic base, a nickel catalyst, a phosphine compound and a solvent. According to the manufacturing method of the present invention, even if a nickel catalyst is used as the catalyst, a desired boronic acid ester compound can be obtained in a sufficiently high yield. Furthermore, even if aryl chloride or aryl bromide having relatively low price and low reactivity, was used as the aryl halide compound, a desired boronic acid ester compound can be obtained in a sufficiently high yield.

Claims23

Dependent claims

A method for preparing a boronic acid ester compound represented by formula (3):

wherein Ar represents an optionally substituted aromatic hydrocarbon group, or an optionally substituted aromatic heterocyclic group;
R represents a an optionally substituted alkylene group, or an optionally substituted arylene group;
characterized by reacting a compound represented by formula (1):
Ar—X (1)
wherein Ar is as defined above,
X represents a halogen atom, an optionally substituted alkylsulfonyloxy group, or an optionally substituted arylsulfonyloxy group;
with a compound represented by formula (2):
wherein R is as defined above;
in the presence of a nitrogen-containing organic base, a nickel catalyst, a phosphine compound and a solvent.

6 more elements

Dependencies are inferred from the claim text.

Method for manufacturing a boronic acid ester compound

Life of this patent

Method for manufacturing a boronic acid ester compound

Life of this patent

Abstract

Claims23