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US 8,138,376 B2Granted
Preparation of (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentanamine
AssigneeJanssen Pharmaceutica NV
InventorsWalter Ferdinand Maria Filliers, Rudy Laurent Maria Broeckx
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Abstract
The present invention relates to an improved process for the preparation of (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentanamine which is an intermediate for the preparation of the analgesic tapentadol.
Claims10
A process for preparing (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethyl-pentanamine, or an acid addition salt thereof, comprising the steps of
- a) acylating (2S,3R)-1-(dimethylamino)-3-(3-methoxyphenyl)-2-methyl-3-pentanol
- with an acylating agent;
- b) hydrogenolysis of the thus obtained compound (III)
- using a transition metal catalyst in a reaction-inert organic solvent in the presence of hydrogen;
- and
- c) optionally converting the thus obtained (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentanamine
- into an acid addition salt.
4 more elements
Dependencies are inferred from the claim text.