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1020180-19-1

1-(4-Bromo-2-methylphenyl)piperidine synthesis

2synthesis methods
-

Yield:1020180-19-1 41.5%

Reaction Conditions:

with sodium carbonate in ethanol at 80; for 48 h;

Steps:

123.1

Following General Scheme 4 above, ethanol (5 ml_), 4-bromo-2-methanyl- analine(0.5g, 2.69mmol), 1 ,5-dibromopentane (0.68 g, 2.69 mmol) and Na2C03 (0.855 g, 8.06 mmol) were added sequentially to a 20-mL vial with a stirring bar. The vial was then sealed and heated to 80°C for 48hrs. After cooling down, the solid was filtered off and the filtrate was concentrated down in vacuo. The crude product was purified by column chromatography (silica gel, 0 to 30% ethyl acetate in hexanes) to give the title intermediate (310 mg, yield: 41.5%) LC- MS: m/z 254 (M+1 ).

References:

WO2012/37108,2012,A1 Location in patent:Page/Page column 187