Process for preparing 2,4-dihydroxypyridine and...

Details Process for preparing 2,4-dihydroxypyridine and... Process for preparing 2,4-dihydroxypyridine and...

C - Chemistry, Metallurgy

07

D

C07D 213/69 (2006.01) C07D 213/61 (2006.01) C07D 213/80 (2006.01) C07D 473/00 (2006.01)

Patent

CA 2241887

The present invention is directed to a process for preparing 2,4-dihydroxypyridine comprising heating a compound of formula A wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed (See formula I) to a process for preparing 2,4-dihydroxy-3-nitropyridine comprising reacting 2,4-dihydroxypyridine with nitric acid. The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischemia, ameliorating ischemic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.

Procédé d'élaboration de 2,4-dihydroxypyridine comprenant l'étape consistant à élever la température d'un composé de la formule (A). Dans cette formule, R est H, un alkyle ou un aralkyle et un acide phosphorique dans lequel le rapport de l'acide phosphorique à l'eau n'est par inférieur à environ 27 à 1 % en poids. L'invention porte également sur un procédé d'élaboration de 2,4-dihydroxy-3-nitropyridine comprenant l'étape consistant à faire réagir 2,4-dihydroxypyridine avec l'acide nitrique. Les procédés de la présente invention permettent d'obtenir des intermédiaires qui sont utiles pour l'élaboration de composés eux-mêmes utiles pour le traitement des maladies cardiovasculaires marquées par l'hypertension ou l'ischémie du myocarde, pour l'amélioration des lésions ischémiques ou de la taille de l'infarctus du myocarde, ou pour le traitement de l'hyperlipidémie ou de l'hypercholestérolémie.

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