C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/261, 260/242
C07D 239/30 (2006.01) C07D 239/34 (2006.01) C07D 239/46 (2006.01) C07D 239/52 (2006.01) C07D 471/04 (2006.01)
Patent
CA 1076573
A B S T R A C T Process for the preparation of a 4-chloro-5- alkoxycarbonyl-2-methoxy-pyrimidine of the formula: Image in which R1 is a lower alkyl radical with 1 to 4 carbon atoms, which comprises the following stages: A) condensation of a salt of O-methylisourea and an inorganic or organic acid, with an alkyl alkoxy- methylenemalonate Image in an aqueous medium and in the presence of an excess of an alkali metal hydroxide. to form the corresponding salt. of the 5-alkoxycarbonyl-4-hydroxy-2-methoxy-pyrimidine, and neutralisation of the said salt by the addition of an inorganic or organic acid, in order to liberate this 5-alkoxycarbonyl-4-hydroxy-2-methoxy-pyrimidine, and Image B) bringing the latter compound, suspended in dimethylformamide, into contact with thionyl chloride, at room temperature, in order to form the corresponding 4-chloro-5-alkoxycarbonyl-2-methoxy-pyrimidine: Image Application to the preparation of 6-ethoxycarbonyl- 8-ethyl-2-methoxy-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine.
276401
Geiger Suzanne
Pesson Marcel
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