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1440519-73-2

2-CHLORO-6-(4-METHOXYBENZYL)-6,7-DIHYDROPYRROLO[3,4-B]PYRIDIN-5-ONE synthesis

7synthesis methods
1093879-99-2 Synthesis
Methyl 6-chloro-2-(chloroMethyl)nicotinate

1093879-99-2
9 suppliers
$60.00/5mg

2393-23-9 Synthesis
4-Methoxybenzylamine

2393-23-9
463 suppliers
$20.00/25g

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Yield:1440519-73-2 55%

Reaction Conditions:

in tetrahydrofuran at 20; for 4 h;

Steps:

A.5 Step 5:

To a solution of (4-methoxyphenyl)methanamine (2.49 g, 18.15 mmol) in tetrahydrofuran (50 mL ) was added methyl 6-chloro-2-(chloromethyl)pyridine-3- carboxylate (4.0 g, 18.17 mmol). The mixture was stirred at room temperature for 4 h. The mixture was concentrated under vacuum. The residue was purified by flash column chromatography with 0-25% ethyl acetate in petroleum ether to afford 2-chloro-6-[(4- methoxyphenyl)methyl]-7H-pyrrolo[3,4-b]pyridin-5-one (2.90 g, 55%) as a yellow solid. MS m/z 289.0 [M+1]+.

References:

WO2022/20342,2022,A1 Location in patent:Page/Page column 40; 57