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7-Bromo-2,4-dichloropyrido[3,2-d]pyrimidine synthesis

6synthesis methods
-

Yield: 91%

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine;trichlorophosphate at 130; for 3 h;

Steps:

1.3 Step three, compound 5
Compound 4 (500mg, 2.08mmol) was dissolved in phosphorus oxychloride (10mL),Add N,N-diisopropylethylamine (DIEA, 538mg, 4.16mmol),The reaction solution was heated to 130°C and stirred for 3 hours.The reaction solution was cooled to room temperature and concentrated and added ice water.Extract with ethyl acetate (3x100mL),The organic phase was washed with saturated sodium chloride solution (100 mL) and then dried with anhydrous sodium sulfate,The organic phase was concentrated and purified by silica gel column chromatography (developing solvent: petroleum ether/ethyl acetate = 3/1) to obtain compound 5 (yellow solid, 522 mg, yield 91%).

References:

CN112390795, 2021, A Location in patent:Paragraph 0194-0195; 0202-0204

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