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4-(Methylsulfonyl)-piperidine HCl synthesis

4synthesis methods
189205-49-0 Synthesis
1-Piperidinecarboxylic acid, 4-(Methylsulfonyl)-, 1,1-diMethylethyl ester

189205-49-0
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Yield:479611-96-6 95%

Reaction Conditions:

with hydrogenchloride in ethyl acetate at 0 - 20;

Steps:

62 Reference Example 62

To a mixture of tert-butyl 4-(methylsulfonyl)piperidine-1-carboxylate (1.5 g) and ethyl acetate (10 mL) was added dropwise a 4N hydrochloric acid·ethyl acetate solution (2.5 mL) with stirring under ice-cooling. After stirring overnight at room temperature, the precipitated crystals were collected by filtration and washed with ethyl acetate to give 4-(methylsulfonyl)piperidine hydrochloride as crystals (1.08 g, yield 95%). Recrystallization from ethanol gave colorless prism crystals. melting point: 271-272°C

References:

EP1486490,2004,A1 Location in patent:Page 46