Introduction of a new synthetic route about 213265-83-9

According to the analysis of related databases, 213265-83-9, the application of this compound in the production field has become more and more popular.

213265-83-9 , The common heterocyclic compound, 213265-83-9, name is 4,6-Dichloro-5-fluoropyrimidine, molecular formula is C4HCl2FN2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

(First Step) 4,6-Dichloro-5-fluoropyrimidine (31.8 g, content: 98.9%) and potassium carbonate (31.5 g) are initially charged in acetone (115 ml), and, at 60 C., admixed dropwise over a period of 6 hours with a solution of 44.9 g of (E)-5,6-dihydro-1,4,2-dioxazin-3-yl-(2-hydroxyphenyl)methanone O-methyloxime in 350 ml of acetone. The mixture is stirred at 60 C. for 2 hours, the acetone is distilled off, the mixture is admixed with methylene chloride and water, the organic phase is separated off, the aqueous phase is extracted with methylene chloride, the organic extracts are combined, washed with 5% NaOH and dried over sodium sulphate and the solvent is distilled off. This gives (E)-{2-[(6-chloro-5-fluoro-4-pyrimidinyl)oxy]phenyl}-(5,6-dihydro-1,4,2,-dioxazin-3-yl)methanone O-methyloxime (68.0 g, content: 95.8%, 94.5% of theory) as a solid.

According to the analysis of related databases, 213265-83-9, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Weintritt, Holger; Stelzer, Uwe; Gayer, Herbert; Hubsch, Walter; US2003/92723; (2003); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia