IP Library Granted Patent US 8,183,294
Granted Patent B2
US 8,183,294 · App. 12/984,279 · Granted May 22, 2012

Process for enantioselective synthesis of single enantiomers of thio-substituted arylmethanesulfinyl derivatives by asymmetric oxidation

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Quick Facts
Patent No.
US 8,183,294
App. No.
12/984,279
Granted
May 22, 2012
Kind
B2
Abstract

The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein Ar, Y, R 1 are as defined in claim 1.

Claims (12)

1. A compound selected from:

(−)2-[2-(3,4-dichlorophenoxy)benzyl]sulphinylacetamide; and

(+)2-[2-(3,4-dichlorophenoxy)benzyl]sulphinylacetamide;

wherein said compound has an enantiomeric excess of more than about 80%.

2. A compound according to claim 1 , wherein said compound is (−)2-[2-(3,4-dichlorophenoxy)benzyl]sulphinylacetamide.

3. A compound according to claim 1 , wherein said compound is (+)2-[2-(3,4-dichlorophenoxy)benzyl]sulphinylacetamide.

4. A compound according to claim 2 , wherein said compound has an enantiomeric excess of more than 90%.

5. A compound according to claim 2 , wherein said compound has an enantiomeric excess of more than 95%.

6. A compound according to claim 2 , wherein said compound has an enantiomeric excess of 99% or more.

7. A compound according to claim 3 , wherein said compound has an enantiomeric excess of more than 90%.

8. A compound according to claim 3 , wherein said compound has an enantiomeric excess of more than 95%.

9. A compound according to claim 3 , wherein said compound has an enantiomeric excess of 99% or more.

Assignments (2)
MERGER Recorded Jan 24, 2013
From: CEPHALON FRANCE
To: TEVA SANTE
Reel/Frame 029692/0457 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 1, 2011
From: PRAT, LAURENCE; NECKEBROCK, OLIVIER; SCHWEIZER, DOMINIQUE; LOUVET, PHILIPPE
To: CEPHALON FRANCE
Reel/Frame 025727/0435 →