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950752-52-0

4-chloro-N-(3-chlorophenyl)pyrimidin-2-amine synthesis

2synthesis methods
2-(3-chloroanilino)-1H-pyrimidin-6-one

158661-60-0
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4-chloro-N-(3-chlorophenyl)pyrimidin-2-amine

950752-52-0
18 suppliers
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Yield: 91%

Reaction Conditions:

with trichlorophosphate at 20 - 70; for 1 h;

Steps:


2-(3-Chloro-phenylamino)-pyrimidine-4-ol (444 mg, 2 mmol) is added in portions to 6 mL phosphorous oxychloride at room temperature. The mixture is heated to 70 0C for 1 hour, cooled and the excess phosphorous oxychloride evaporated under reduced pressure. The residue is dissolved in ethyl acetate washed with saturated sodium carbonate solution and brine, dried over sodium sulfate and evaporated. The title compound is obtained in 91 % yield (440 mg): m.p. 112-1 14 0C; MS (ES+) m/z (M + H)+1 240,242.

References:

NOVARTIS AG;NOVARTIS PHARMA GMBH WO2007/109045, 2007, A1 Location in patent:Page/Page column 31-32