反应详情

In analogy to the procedure described for the preparation of example 13, 1,3-dimethyl-6-oxo-5-(3-trifluoromethyl-phenyl)-1,6-dihydro-pyridine-2-carboxylic acid [prepared by i) reaction of 6-hydroxy-3-methyl-5-(3-trifluoromethyl-phenyl)-pyridine-2-carboxylic acid methyl ester; 3-methyl-6-oxo-5-(3-trifluoromethyl-phenyl)-1,6-dihydro-pyridine-2-carboxylic acid methyl ester (tautomers, intermediate 15B) with methyl iodide, cesium carbonate in DMF in analogy to the procedure described for the preparation of intermediate 5F; ii) saponification of the thus formed 1,3-dimethyl-6-oxo-5-(3-trifluoromethyl-phenyl)-1,6-dihydro-pyridine-2-carboxylic acid methyl ester with lithium hydroxide in THF/MeOH in analogy to the procedure described for the preparation of intermediate 5G] was reacted with oxalyl chloride/DMF in CH2Cl2 followed by treatment with 4-pyrrolidin-1-yl-piperidine to give the title compound as colorless solid. MS: 448.2 (MH+).

1. customprepared by i)