Triazolopyridines
A compound, selected technology, applied in 24826A1 discloses a substituted, preparation of pharmaceutical compositions for treating or preventing diseases, and the field of intermediate compounds for preparing the compounds, which can solve problems such as low hydrolysis stability
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Embodiment 011
[1146] N , N -Diethyl-4-{[6-(4-{[(4-fluorophenyl)acetyl]amino}phenyl)[1,2,4]triazolo[1,5- a ]pyridin-2-yl]amino}-3-methoxybenzamide
[1147]
[1148] Towards Int3.4 (150 mg) in a stirred suspension of toluene (3.5 mL) and NMP (0.5 mL), was added 4-bromo- N , N -Diethyl-3-methoxybenzamide (237mg), Pd 2 dba 3 (19mg) and rac-BINAP (26mg). The flask was degassed twice and backfilled with argon. The mixture was stirred at room temperature for 5 minutes. Cesium carbonate (405 mg) was added, the flask was degassed twice and backfilled with argon, and the mixture was heated to reflux for 20 h. Water was added, and the reaction mixture was extracted with ethyl acetate. The organic phase was washed with saturated sodium chloride solution, dried (sodium sulfate) and the solvent was removed in vacuo. Chromatography on silica gel gave a solid which was triturated with cyclohexane to give 27 mg of the title compound.
[1149]
[1150] from intermediate Int3.4 start with...
Embodiment 012
[1152] N -(4-{2-[(4-cyano-2-methoxyphenyl)amino][1,2,4]triazolo[1,5- a ]pyridin-6-yl}phenyl)-2-(4-fluorophenyl)acetamide
[1153]
[1154]
[1155] Starting Materials: Intermediates Int3.4 ; 4-Bromo-3-methoxybenzonitrile.
Embodiment 013
[1157] N -(4-{2-[(2-ethoxy-4-fluorophenyl)amino][1,2,4]triazolo[1,5- a ]pyridin-6-yl}phenyl)-2-(4-fluorophenyl)acetamide
[1158]
[1159]
[1160] Starting Materials: Intermediates Int3.4 ; 1-Bromo-2-ethoxy-4-fluorobenzene.
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