Patent ID: 7777045
Filing Date: 2010-08-17
Classification: C07D

Abstract:
1. A process for the preparation of a 2-ethylaminopyridine derivative of general formula (I) or a salt thereof in which: p is an integer equal to 1, 2, 3 or 4; X is independently selected from the group consisting of a hydrogen atom, a halogen atom, a nitro group, a cyano group, a hydroxy group, an amino group, a sulfanyl group, a pentafluoro-λ said process comprising: (A) a first step according to reaction scheme 1 in which: X and p are as defined above; R is a C Hal represents a halogen atom; comprising: to provide a 2-methylcyanopyridine derivative; wherein said first step (A) is conducted at a temperature of from 0° C. to reflux; (B) a second step according to reaction scheme 2: in which: X and p are as defined above; R R2 represents a halogen atom or a —OCOAlk group; and Alk represents a C comprising the catalytic reduction of reaction of a 2-methylcyanopyridine derivative obtained in the first step in the presence of an acylating agent of formula R 1 COR 2 and of a catalyst, in a solvent, under a hydrogen pressure of from 4 to 40 bar, to provide a 2-ethylaminopyridyl derivative; (C) a third step according to reaction scheme 3: in which: X and p are as defined above; and R comprising the hydrolysis in water of a 2-ethylaminopyridine derivative obtained in the second step by adding to it from 1 to 20 molar equivalent of an acid, at a temperature of from 20° C. to reflux, to provide a compound of general formula (I).