Process for the preparation on 2-aminomethylpyridine derivatives
AssigneeBayer CropScience AG
InventorsJorn Stolting, Brian Burton
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Abstract
The present invention relates to a novel process for the preparation of 2-amino-methylpyridine derivatives of the formula (I), comprising reacting in a first step 2-substituted pyridine derivatives of the formula (II), with a nitroalkane of the formula (III), in the presence of a base resulting in 2-nitromethylpyridine derivatives of the formula (IV) and hydrogenating these 2-nitromethylpyridine derivatives of the formula (IV) in a second step in the presence of a catalyst and in the presence of an acid, where in the formulae n, X, Y, R1, R2 and A are as defined in the description.
Claims12
A process for the preparation of 2-aminomethylpyridine derivatives of formula (I) or salts thereof
- comprising the steps of reacting 2-substituted pyridine derivatives of the formula (II)
- with a nitroalkane of the formula (III)
- in the presence of a base resulting in 2-nitromethylpyridine derivatives of the formula (IV)
- and then hydrogenating these 2-nitromethylpyridine derivatives of the formula (IV) in the presence of a catalyst and an acid,
- wherein
- n represents 0, 1, 2 or 3,
- X represents a halogen atom,
- Y is selected from the group consisting of a halogen atom, halogenoalkyl, alkoxycarbonyl, and alkylsulfonyl, where each Y may be identical or different if n represents, 2 or 3,
- R1 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, and cycloalkylmethyl,
- R2 is selected from the group consisting of hydrogen and alkyl, or
- R1 and R2 taken together can represent alkylene, and
- A is selected from the group consisting of halogen, trifluoromethylsulfonyl methylsulphonyl, and other radicals that can act as negatively charged leaving groups.
Dependencies are inferred from the claim text.