January 7, 2013

CAS databases provide millions of journal article references from more than 10,000 major scientific journals worldwide, patent and patent family references from 63 patent authorities around the world, and other reputable web sources.  

The following patent record is from the CAplusSM database.

CAPLUS COPYRIGHT 2013 ACS

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

Abstract:

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.

Recent News

    
    October 7, 2014 | CAS and Obiter Research form a
    multi-year collaboration to provide SciFinder to their
    research team
    
    September 29, 2014
| Cooperative Patent Classification
    (CPC) Combination Set Data Now Available in CAplus,
    INPADOCDB and USPAT Databases
         
    September 22, 2014
| STN Global Value Pricing
    Agreement Supports the Swedish Patent and
    Registration Office in Providing High Quality and
    Efficient Examination
    
 
                                                                     More News >> 

 Media Contact

 Name: Rhonda Ross
 Phone: 614-447-3624                                       
 Email: cas-pr@cas.org