| 摘要 |
The invention provides a production method of a biaryl compound of the formula [3] or a salt thereof, including reacting a 2-phenylazole derivative of the formula [1] or a salt thereof, with a benzene derivative of the formula [2] or a salt thereof in the presence of a metal catalyst, a base, and one or more of (a) a monocarboxylic acid metal salt, (b) a dicarboxylic acid metal salt, (c) a sulfonic acid metal salt, and (d) a phosphate or phosphoric amide metal salt represented by RAxP(O)(OM)y;;wherein each symbol is as defined herein. |
| 主权项 |
1. A method of producing a biaryl compound represented by the formula [3]:wherein R1 to R4 are each independently a hydrogen atom, or an alkyl group, an aralkyl group or an aryl group, each of which optionally has substituent(s), R5 is an alkyl group, an aralkyl group or an aryl group, each of which optionally has substituent(s), m is an integer of 0 to 5, and ring A is an optionally substituted nitrogen-containing heterocycle,
or a salt thereof, comprising reacting a 2-phenylazole derivative represented by the formula [1]:wherein each symbol is as defined above, or a salt thereof with a benzene derivative represented by the formula [2]:wherein R5 and m are as defined above, and X1 is a leaving group,
in the presence of a metal catalyst, a base and one or more kinds of compounds selected from the group consisting of the following (a)-(d); (a) a monocarboxylic acid metal salt (b) a dicarboxylic acid metal salt (c) a sulfonic acid metal salt, and (d) a phosphate or phosphoric amide metal salt represented by RAxP(O)(OM)y wherein RA is R′″O or R′″2N (wherein R′″ is a hydrogen atom, or a straight chain or branched chain alkyl group having 1-20 carbon atoms, an aralkyl group having 7-14 carbon atoms or an aryl group having 6-18 carbon atoms, each of which optionally contains a nitrogen atom, an oxygen atom or a sulfur atom), M is a metal atom, x and y are each independently an integer of 1 or 2, and x+y is 3. |
