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(4-(Piperidin-1-ylsulfonyl)phenyl)MethanaMine synthesis

3synthesis methods
227935-30-0 Synthesis
4-(piperidine-1-sulfonyl)benzonitrile

227935-30-0
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Yield:205259-71-8 25%

Reaction Conditions:

with ammonium hydroxide;hydrogen in methanol;water at 20; under 760.051 Torr;

Steps:

5.2 Step 2. 4-(Piperidine-1-sulfonyl)-benzylamine

To a solution of 4-(piperidine-1-sulfonyl)-benzonitrile (2 g, 7,83 mmol, 1.00 equiv) in methanol (40 mL) was added Raney Ni (0.2 g, 0. 10 equiv) and ammonium hydroxide (4 mL, 28-30% aqueous solution) The reaction mixture was stirred under 1 atmosphere of hydrogen overnight at rt, The catalyst was removed by filtration. The filtrate was concentrated under vacuum and the residue was purified on a silica gel column eluted with dichloromethane/methanol ( 1/30) to give 500 mg (25%) of the title compound as a light yellow oil. LC/MS (Method H, ESI): RT = 1 .08 mm, m/z = 255.0 [M + H]+ .

References:

WO2013/127266,2013,A1 Location in patent:Page/Page column 146; 147