Process for preparing 4-(cyclopropylmethoxy)-N-(3,5-dichloro-1-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide

摘要

The present invention relates to a novel process for preparing the compound 4-(cyclopropylmethoxy)-N-(3,5-di-chloro-1-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide of formula (1), in base or hydrate form or in the form of pharmaceutically acceptable salts, and also to several novel synthetic intermediates that are useful in this preparation process.;

主权项

1. A process for preparing 4-(cyclopropylmethoxy)-N-(3,5-dichloro-1-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide, in base or hydrate form or in the form of a pharmaceutically acceptable salt, of formula 1 below:wherein the process comprises:
a step c): reaction of the compound 2-hydroxymethyl-5-methoxy-4-pyrid-(1H)-one of formula 5 with methylcyclopropane bromide and a base, in a polar aprotic solvent, according to the scheme below: a step b): oxidation reaction of compound 4 obtained in step c), according to the scheme below:and
a step a): coupling reaction of compound 2 obtained in step b) with 3,5-dichloroaminopyridine N-oxide (compound 3) or N-Boc-dichloropyridoxide (compound 3a), according to the scheme below: