Methyl (1-benzyl-4-Methylpiperidin-3-yl)carbaMate synthesis

Yield:1206875-41-3 66%

Reaction Conditions:

with hydrogen;platinum(IV) oxide in methanol at 60; for 16 h;

Steps:

1.5

Step 5O o_/ N_x N^" "or ^ N_x^JN^' O H H[00155] Methyl l-benzyl-4-methylpiperidin-3-yl-carbamate: Platinum oxide (1.0 g, 4.41 mmol, 0.11 equiv.) was added to a solution of methyl l-benzyl-4- methyl- 1,2, 5, 6-tetrahydropyndin-3-ylcarbamate (10 g, 38.46 mmol, 1.00 equiv.) in methanol (200 mL). After introducing hydrogen gas, the mixture was stirred at about 60 ⁰C for about 16 hours and then was filtered. The resulting filtrate was concentrated to give a crude residue that was then purified by silica gel column chromatography (ethyl acetate / petroleum (1:2)) to afford the title product a yellow solid (7 g; yield = 66%). LC-MS: m/z = 263 (M+H)⁺.

References:

WO2010/123919,2010,A2 Location in patent:Page/Page column 50-51