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US 8,802,857 B2Granted
Process for preparing 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compounds
AssigneeTheravance Biopharma R&D IP, LLC
InventorsEric L. Stangeland, Miroslav Rapta
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Abstract
The invention relates to processes and intermediates for preparing compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors.
Claims4
A process for preparing a compound of formula 1:
- or a salt thereof, where L is a sulfonic ester group having the formula —OS(O2)—R, where R is —C1-4-alkyl or phenyl, and the phenyl group is optionally substituted with —C1-4-alkyl, halo or nitro;
- and P is an amino-protecting group;
- the process comprising the steps of:
- (a′) reacting a compound of formula 4:
- or a salt thereof, with a reducing agent to provide a compound of formula 5:
- or a salt thereof;
- and
- (b′) converting the hydroxyl group of the compound of formula 5 or a salt thereof, into a sulfonic ester group, L, to provide a compound of formula 1 or a salt thereof.
5 more elements
Dependencies are inferred from the claim text.