2,3-Dichloro-5,6-dicyano-1,4-benzoquinone → Methyl 3-hydroxy-4-oxo-6,7,-dihydro-4h-pyrido[1,2-a]pyrimidine-2-carboxylate

Participants

Reaction Conditions

Reaction Steps

To a solution of methyl 3-hydroxy-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-2-carboxylate in 1,4,-dioxane was added dichloro-dicyano benzoquinone (1.1 eqs.). The mixture was stirred and heated to 60° C. for 1 hour. TEA (5 eqs.) was added and stirring was continued for 4 hours. The solution was cooled to room temperature and the product was purified by preparative RP-HPLC, using water (0.1% TFA) and acetonitrile (0.1% TFA) as eluants (column: C18). The product was obtained after lyophilization of the pooled product fractions as a fluffy white material.

Provenance & Evidence