Novel process for the preparation of roflumilast

Details Novel process for the preparation of roflumilast Novel process for the preparation of roflumilast

C - Chemistry, Metallurgy

07

D

C07D 213/75 (2006.01)

Patent

CA 2503290

The invention relates to novel processes for the preparation of high-purity roflumilast. The process involves reacting the anion of 4 - armino -3,5 dichloropyridine (I), with an activated derivative of 3-cyclopropylmethoxy-4- difluoromethoxybenzoic acid (II), characterized in that the molar ratio of the employed anion of 4-amino-3,5 dichloropyridine to the activated derivative of 3-cyclopropylmethoxy-4-difluoromethoxybenzoic acid is at least 1.5 and at most 3, preferably at least 1.8 and at most 2.7 particularly preferably at least 2 and at most 2.5 and very particularly preferably 2.2

L'invention concerne de nouveaux procédés de préparation de roflumilast très pur. Le procédé consiste à faire réagir l'anion de 4 - armino -3,5 dichloropyridine (I), avec un dérivé activé d'acide 3-cyclopropylméthoxy-4-difluorométhoxybenzoïque (II), et caractérisé en ce que le rapport molaire entre l'anion employé de 4-amino-3,5 dichloropyridine et le dérivé activé d'acide 3-cyclopropylméthoxy-4-difluorométhoxybenzoïque est d'au moins 1,5 et au plus 3, de préférence au moins 1,8 et au plus 2,7, idéalement au moins 2 et au plus 2,5 et de façon plus particulièrement préférentielle 2,2.

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