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1292317-56-6

D0128 synthesis

2synthesis methods
40530-18-5 Synthesis
5-Bromo-2-hydroxybenzonitrile

40530-18-5
185 suppliers
$15.00/1g

109384-19-2 Synthesis
N-BOC-4-Hydroxypiperidine

109384-19-2
346 suppliers
$5.00/1g

D0128

1292317-56-6
19 suppliers
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Yield:1292317-56-6 89.2%

Reaction Conditions:

with triphenylphosphine;diethylazodicarboxylate in tetrahydrofuran at 20; for 18 h;

Steps:

I-5.1

To a solution of 5-bromo-2-hydroxy-benzonitrile (1.98 g, 10.0 mmol) in dry THF (40 mL) was added tert-butyl 4-hydroxypiperidine-l-carboxylate (2.41 g, 12 mmol), PPh3 (3.14 g, 12 mmol), followed by addition of DEAD (1.89 mL, 12 mmol) at rt. After stirring at rt for 18 h, the reaction mixture was concentrated under reduced pressure. The residue was purified by column chromatography (Si02, EtOAc/Hexanes, 0-80%) to afford the title compound (3.4 g, 89.2%).

References:

WO2011/46970,2011,A1 Location in patent:Page/Page column 96

40530-18-5 Synthesis
5-Bromo-2-hydroxybenzonitrile

40530-18-5
185 suppliers
$15.00/1g

141699-59-4 Synthesis
1-Boc-4-methanesulfonyloxypiperidine

141699-59-4
199 suppliers
$6.00/1g

D0128

1292317-56-6
19 suppliers
inquiry