2-Amino-5-fluorophenol → N-(4-fluoro-2-hydroxyphenyl)-2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydro-pyrimidin-2-yl]acetamide

Participants

Reaction Steps

The product is prepared according to the procedure described in Stage 1 of Example 2, using 550 mg of sodium [4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate and 815 mg of 2-amino-5-fluorophenol in place of 2-aminophenol. After purification by silica gel column chromatography, elution being carried out with pure CH2Cl2 then CH2Cl2/MeOH: 95/05, 149 mg of N-(4-fluoro-2-hydroxyphenyl)-2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetamide obtained in the form of a grey solid, the characteristics of which are the following:

Provenance & Evidence