IP Library Granted Patent US 6,946,269
Granted Patent B2
US 6,946,269 · App. 10/727,475 · Granted Sep 20, 2005

Alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid of use as intermediates

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Quick Facts
Patent No.
US 6,946,269
App. No.
10/727,475
Granted
Sep 20, 2005
Kind
B2
Abstract

The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.

Claims (18)

1. A process for the preparation of a compound of formula:

in which R 1 represents a linear C 1 -C 4 -alkyl and X represents a halogen which comprises treating, with an enzyme, a compound of formula:

2. A process according to claim 1 wherein the enzyme is chosen from lipases, esterases and proteases.

3. A process according to claim 2 wherein the enzyme is Candida cylindracea or Candida rugosa lipase or esterase, separately or as a mixture.

4. A compound of formula:

wherein X represents a halogen, and R 1 represents a linear C 1 -C 4 -alkyl.

5. A compound of formula:

in which X represents a halogen.

6. A process for the preparation of a compound of formula (VII):

wherein X represents a halogen, which comprises hydrolyzing a compound of S configuration corresponding to the formula

in which X represents a halogen and R 1 represents a linear C 1 -C 4 alkyl.

7. A process for the preparation of a compound of formula (VIII):

wherein X represents a halogen, which comprises reducing a compound of S configuration corresponding to the formula

in which X represents a halogen and R 1 represents a linear C 1 -C 4 alkyl in the presence of a reducing agent.

8. A process for the preparation of a compound of the formula (IX):

wherein X represents a halogen, which comprises reducing a compound according to claim 4 in the presence of an alkaline hydride.

9. A process for the preparation of a compound of formula (X):

wherein X represents a halogen, which comprises cyclizing a compound according to claim 5 .

Assignments (2)
CHANGE OF NAME Recorded Jul 22, 2005
From: SANOFI-SYNTHELABO
To: SANOFI-AVENTIS
Reel/Frame 016345/0189 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 22, 2005
From: CASTRO, BERTRAND; DORMOY, JEAN-ROBERT; RABION, ALAIN
To: SANOFI-SYNTHELABO
Reel/Frame 016170/0747 →