Ethyl chloroformate → HCID 13885671, compound

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Reaction Steps

A mixture of 2.06 g of ethyl 2-ethoxycarbonylaminonicotinate (m.p. 60°, obtainable by boiling ethyl 2-aminonicotinate with ethyl chloroformate for 5 h in the presence of N,N-diisopropylethylamine in toluene) and 2.54 g of 1-(2-aminoethyl)-4-p-fluorobenzoylpiperidine (Rf 0.43 on silica gel with butanol/ethanol/water/ethyl acetate/acetic acid 50:50:50:25:25) is heated at 190° for 1 h. The mixture is cooled and taken up in methanol and, on cooling, 3-[2-(4-p-fluorobenzoylpiperidino)ethyl]-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine is obtained, m.p. 237°. Hydrochloride m.p. 297°-298°. Fumarate m.p. 253°-255°.

Provenance & Evidence