IP Library Granted Patent US 8,859,812
Granted Patent B2
US 8,859,812 · App. 13/394,693 · Granted Oct 14, 2014

Compound reagents and method for synthesizing enantiomerically enriched amino acids

Inventors: Eric N. Jacobsen (Cambridge, MA); Stephan J. Zuend (Mannheim, DE)
Assignee: President and Fellows of Harvard College
C07C253/08C07C2101/16C07C2103/74C07D307/52C07D333/20C07C227/26C07C335/16C07C2101/14
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Quick Facts
Patent No.
US 8,859,812
App. No.
13/394,693
Granted
Oct 14, 2014
Kind
B2
Abstract

Described herein are compounds of formula (I), related compositions, and their use, for example in the formation of α-amino acids or a precursor thereof such as an α-aminonitrile.

Claims (23)

1. A compound or pharmaceutically acceptable salt thereof selected from the formula (I):

wherein

X is selected from O, S and NR 5 ;

R 1a and R 1b is optionally substituted aryl;

R 2 is hydrogen, optionally substituted alkyl;

R 3 is optionally substituted alkyl, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted aralkyl, optionally substituted heteroaralkyl, or optionally substituted heterocyclylalkyl;

R 4 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted heteroaralkyl, optionally substituted aralkyl or optionally substituted heterocyclylalkyl;

R 5 is hydrogen, alkyl, aryl, or arylalkyl.

2. The compound of claim 1 , wherein the compound of formula (I) is enantiomerically enriched for the R isoform.

3. The compound of claim 1 , wherein the compound is a compound of formula (Ia)

wherein the compound has an enantiomeric excess (ee) of at least about 50%.

4. The compound of claim 1 , wherein the compound is a compound of formula (Ib)

wherein the compound has an ee of at least about 50%.

5. The compound of claim 1 , wherein the compound of formula (I) is enantiomerically enriched for the S isoform.

6. The compound of claim 1 , wherein X is selected from O and S.

7. The compound of claim 6 , wherein X is S.

8. The compound of claim 1 , wherein R 1a is phenyl.

9. The compound of claim 1 , wherein R 1b is phenyl.

10. The compound of claim 1 , wherein the compound of formula (I) is selected from a compound of formula (Ic):

11. The compound of claim 1 , wherein the compound of formula (I) is selected from a compound of formula (Id):

wherein X 1 , X 2 , Y 1 and Y 2 are each independently selected from hydrogen, alkyl, alkoxy or haloalkyl.

12. The compound of claim 11 , wherein Y 1 or Y 2 is haloalkyl.

13. The compound of claim 1 , wherein the compound of formula (I) is

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 10, 2012
From: JACOBSEN, ERIC N.; ZUEND, STEPHAN J.
To: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
Reel/Frame 029108/0107 →
CONFIRMATORY LICENSE Recorded Mar 16, 2012
From: HARVARD UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 027874/0449 →
Continuity (2)
Provisional Application 61240558 · Sep 8, 2009
Related Publication 20130066109A1 · Mar 14, 2013