IP Library Granted Patent US 9,272,983
Granted Patent B2
US 9,272,983 · App. 13/502,144 · Granted Mar 1, 2016

2-amino-3-methyl-hex-5-enoic acid and its use in the production of peptides including bacitracins

Inventors: Martin Mansson (Oslo, NO); Christine Senstad (Hosle, NO); Jon Efskind (Oslo, NO); Vidar Bjornstad (Sorumsand, NO)
Assignee: XELLIA PHARMACEUTICALS APS
C07C229/08C07C229/30C07K7/58
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Quick Facts
Patent No.
US 9,272,983
App. No.
13/502,144
Granted
Mar 1, 2016
Kind
B2
Abstract

The present invention concerns 2-amino-3-methyl-hex-5-enoic acid, its use for the production of peptides such as bacitracins and a method for producing it.

Claims (11)

1. The compound 2-amino-3-methyl-hex-5-enoic acid.

2. A compound according to claim 1 having (2S,3S) configuration.

3. A compound according to claim 1 having (2R,3S) configuration.

4. A compound according to claim 1 having (2S,3R) configuration.

5. A compound according to claim 1 having (2R,3R) configuration.

6. A method of producing a compound according to claim 1 , comprising a cross coupling of a vinyl Grignard agent with valine having a halide in 4-position.

7. The method according to claim 6 , where the cross coupling is catalyzed by Li 2 CuCl 4 .

8. A method of producing a compound according to claim 1 , comprising the following steps:

(a) coupling a vinyl Grignard reagent with 4-Iodo-N-phathaloylvaline methyl ester to form 2-(1,3-dioxo-1,3-dihydroisoindol-2-yl)-3-methyl-hex-5-enoic acid methyl ester,

(b) cleaving the methyl ester moiety to generate the corresponding carboxylic acid; and

(c) deprotecting the alpha-amino group of 2-amino-3-methyl-hex-5-enoic acid.

Assignments (2)
CHANGE OF NAME Recorded Apr 24, 2012
From: AXELLIA PHARMACEUTICALS APS
To: XELLIA PHARMACEUTICALS APS
Reel/Frame 028093/0980 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2012
From: MANSSON, MARTIN; SENSTAD, CHRISTINE; EFSKIND, JON; BJORNSTAD, VIDAR
To: AXELLIA PHARMACEUTICALS APS
Reel/Frame 028050/0180 →
Continuity (2)
Provisional Application 61255521 · Oct 28, 2009
Related Publication 20120202968A1 · Aug 9, 2012