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1303973-24-1

tert-butyl 4,4-difluoro-3-(hydroxyMethyl)piperidine-1-carboxylate synthesis

5synthesis methods
24424-99-5 Synthesis
Di-tert-butyl dicarbonate

24424-99-5
863 suppliers
$13.50/25G

1331775-99-5 Synthesis
(4,4-difluoropiperidin-3-yl)Methanol hydrochloride

1331775-99-5
23 suppliers
$45.00/2.5mg

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Yield:-

Reaction Conditions:

with sodium hydrogencarbonate in dichloromethane at 20; for 2 h;

Steps:

39

A mixture of (4,4-difluoro-piperidin-3-yl)-methanol chloride (2.6 mmol, 0.4g), Boc anhydride (3.2 mmol, 0.7g) in 6 ml_ of saturated sodium bicarbonate and 12 mL of DCM was stirred at room temperature for 2 h. The mixture was evaporated, diluted with DCM, washed with brine, dried, evaporated, and the resulting residue was chromatographed with 20:1 hexane/EtOAc afforded 4,4- difluoro-3-hydroxymethyl-piperidine-1-carboxylic acid tert-butyl ester (520 mg).

References:

WO2011/103091,2011,A1 Location in patent:Page/Page column 95