| 摘要 |
PROBLEM TO BE SOLVED: To provide a new method for producing 2-halogenated benzamides, capable of economically advantageously producing the 2-halogenated benzamide having a sulfonyl on its amide side chain. SOLUTION: This method for producing 2-halogenated benzamides comprises reacting a benzamide of formula (II) [R<SP>1</SP>, R<SP>2</SP>, R<SP>3</SP>, R<SP>4</SP>and R<SP>6</SP>are each H, a 1-6C alkyl; R<SP>5</SP>is a 1-6C alkyl; Y<SP>1</SP>, Y<SP>2</SP>, Y<SP>3</SP>and Y<SP>4</SP>are each H, a halogen, CN, nitro, a 1-6C alkyl, a 1-6C alkylcarbonyl, carboxyl, (substituted) phenylcarbonyl, (substituted) benzylcarbonyl, -CON(R<SP>7</SP>)R<SP>8</SP>, -N(R<SP>7</SP>)-COR<SP>8</SP>, (substituted) phenyl or the like; k is 1 or 2; and m is 0 or 1] with a halogenating agent in the presence of a Pd catalyst to form a substituted benzamide of formula (III) (X is Cl, Br or I) and then reacting the substituted benzamide with an oxidizing agent to produce the 2-halogenated benzamide expressed by formula (I). COPYRIGHT: (C)2005,JPO&NCIPI
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