January 7, 2013

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The following patent record is from the CAplusSM database.


Patent Number: US 8299305
Title: Process for preparation of atomoxetine  
Inventor(s): Chen, Bo-Fong; Li, Yan-Wei; Yeh, Jinun-Ban; Wong, Wei-Chyun
Patent Assignee(s): SCI Pharmtech, Inc., Taiwan
Source: U.S. Pat. Appl. Publ., 6pp. CODEN: USXXCO
Language: English


This invention provides a process for the preparation of atomoxetine, which comprises Mannich reaction of acetophenone, formaldehyde, and methylhydroxylamines HNMe(OR) [wherein R is H, alkyl, or aryl] to give the corresponding amino ketones Ph(C=O)(CH2)2NMe(OR) [wherein R is the same as defined above], followed by enantioselective reduction to afford the intermediate (R)-PhCH(OH)(CH2)2NMe(OR) [wherein an absolute configuration of a chiral center is R], which undergoes reductive N,O-cleavage reaction and ether formation with 2-fluorotoluene. For example, Mannich reaction of N,O-dimethylhydroxylamine hydrochloride, paraformaldehyde, and acetophenone gave 3-(N-methoxy-N-methylamino)-1-phenyl-1-propanone hydrochloride salt in 87.6% yield, followed by RuCl2-((S)-DMSEGPHOS)((S)-DAIPEN)-catalyzed asym. hydrogenation to afford (R)-3-(N-methoxy-N-methylamino)-1-phenyl-1-propanol in 98.8% yield and 99% ee, which underwent Raney-nickel-catalyzed reductive N,O-cleavage reaction and etherification with 2-fluorotoluene. The present invention provides an improved and industrially advantageous method for preparing atomoxetine.

View the full-text patent here.

Note: Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced the abstract using additional information found in the patent.

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