C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/228, 260/296
C07D 213/81 (2006.01) A61K 31/44 (2006.01)
Patent
CA 1330802
Abstract of the disclosure: An improved process for the preparation of N,N'-bis- (alkoxyalkyl)-pyridine-2,4-dicarboxamides The invention relates to an improved process for the preparation of N,N'-bis(alkoxyalkyl)-pyridine-2,4-di- carboxamides and to the use of these compounds for the preparation of pharmaceuticals which can be administered orally. In the process according to the invention the compounds of the formula I Image (I) in which R1 denotes C1-C4-alkyl which is monosubstituted by C1-C4-alkoxy are obtained by firstly A) reacting pyridine-2,4-dicarboxylic acid in toluene with a 2-3-fold excess of SOCl2 at temperatures of 90-110°C, dissolving the resulting intermediate in dioxane, and B) adding dioxane to 4 times the molar amount of alkoxyalkylamine of the formula II Image (II) in which R2 denotes C1-C4-alkylene and R3 denotes C1-C4-alkyl, and subsequently, at a temperature of -5 to +5°C, either adding the solution prepared as in A) drop- wise to the solution prepared as in B), or adding the solution prepared as in B) dropwise to the solution prepared as in A), and reaction subsequently being allowed to take place at room temperature.
607509
Baader Ekkehard
Bickel Martin
Burghard Harald
Gunzler-Pukall Volkmar
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Hoechst Aktiengesellschaft
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