Novel process for the preparation of 2-aminomethylpyrimidine derivatives

Process for the preparation of 2-aminomethylpyridine derivatives of general formula (I) or a salts thereof

• in which
• n represents 0, 1, 2 or 3,
• X represents a halogen atom,
• Y represents a halogen atom, halogenoalkyl, alkoxycarbonyl or alkylsulphonyl, where Y may be identical or different, if n represents 2 or 3,
• R1 represents hydrogen, alkyl, cycloalkyl or cycloalkylmethyl,
• R2 represents hydrogen or alkyl,
• R1 and R2 furthermore together represent alkylene,
• comprising reacting in a first step 2-substituted pyridine derivatives of the formula (II)
• in which
• n, X and Y are as defined above and
• A represents a halogen atom, trifluoromethylsulphonyl or methylsulphonyl, or any other radical which may act as a negatively charged leaving group,
• with a nitroalkane of the formula (III)
• in which
• R1 and R2 are as defined above,
• in the presence of a base resulting in 2-nitromethylpyridine derivatives of the formula (IV)
• in which
• n, X, Y, R1 and R2 are as defined above,
• 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.