Cesium carbonate → 4-[6-(5-Chloro-2-fluoro-phenyl)-3-methyl-isoxazolo[5,4-d]pyrimidin-4-ylamino]-nicotinic acid methyl ester

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Reaction Conditions

Reaction Steps

4-Chloro-6-(5-chloro-2-fluoro-phenyl)-3-methyl-isoxazolo[5,4-d]pyrimidine (prepared by method used for compound of formula (43) (298 mg, 1 mmole) was dissolved in dioxane (4 ml), and BINAP (4.67 mg, 0.0075 mmole), 4-Amino-nicotinic acid methyl ester (182 mg, 1.2 mmole), cesium carbonate (456 mg, 1.4 mmole), and Pd2(dba)3 (2.29 mg, 0.0025 mmole) were added to the mixture and heated to 90° C. overnight. Dioxane was removed under vacuum and the residue was triturated with ethyl acetate (5 ml) and the product was isolated by filtration. 525 mg of solid were obtained which also contained cesium carbonate as by-product.

Provenance & Evidence