8-chloro-3H-pyrido[3,4-d]pyrimidin-4-one synthesis

6synthesis methods

Product Name:8-chloro-3H-pyrido[3,4-d]pyrimidin-4-one
CAS Number:84341-13-9
Molecular formula:C7H4ClN3O
Molecular Weight:181.58

58483-94-6 Synthesis

3-Amino-2-chloropyridine-4-carboxylic acid

58483-94-6
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8-chloro-3H-pyrido[3,4-d]pyrimidin-4-one

84341-13-9
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$101.00/50mg

Yield:84341-13-9 85%

Reaction Conditions:

in butan-1-ol at 130; for 16 h;

Steps:

8-chloropyrido[3,4-d]pyrimidin-4(3H)-one:

Formamidine acetate (1.75 g, 16.80 mmol) was added to a suspension of 3-amino-2-chloroisonicotinic acid (580 mg, 3.36 mmol) in butan-l-ol (20 mL) and the mixture was stirred at 130°C for 16 h. The reaction mixture was cooled down and the precipitate was collected by filtration to give the title compound as an off-white solid (520 mg, 85%). 1H NMR (400 MHz, DMSO-d6) d: 12.80 (br s, 1H), 8.42 (d, 7=5.2 Hz, 1H), 8.32 (s, 1H), 7.97 (d, 7=5.2, Hz, 1H).

References:

WO2020/163193,2020,A1 Location in patent:Paragraph 00247