4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compounds
Inventors
Patterson, Lori Jean • Stangeland, Eric L.
Assignees
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Publication Number
US-11723900-B2
Publication Date
2023-08-15
Expiration Date
Abstract
The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Core Innovation
The disclosed invention concerns processes for preparing the hydrochloride salt of a compound of formula 1, identified as 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine hydrochloride. The claims describe two approaches to obtaining the salt: hydrochloride-salt formation using hydrochloric acid, and salt formation using a reaction mixture associated with acetyl chloride and ethanol. The examples identify the product as a crystalline salt material and report purity above 99%.
The supplied content does not include the patent's abstract, summary, or background section, so the problem being solved is not explicitly described. The claims distinguish two approaches to obtaining the same hydrochloride salt, and the example summary mentions related fluorinated piperidine analogs alongside SERT and NET binding thresholds without providing a claim-specific process-performance comparison.
Claims Coverage
The two independent claims cover distinct approaches for preparing the hydrochloride salt of a compound of formula 1. The claim set contains two inventive features.
Hydrochloride salt formation using hydrochloric acid
The first independent claim covers preparing the hydrochloride salt of a compound of formula 1 through hydrochloric acid-based salt formation.
Hydrochloride salt formation using an acetyl chloride and ethanol reaction mixture
The second independent claim covers preparing the hydrochloride salt of a compound of formula 1 using a reaction mixture associated with acetyl chloride and ethanol.
The independent claims cover two approaches to preparing the same hydrochloride salt. The dependent claims further specify solvent or isolation features.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Preparation of the hydrochloride salt of a compound of formula 1.
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