IP Library Granted Patent US 6,858,738
Granted Patent B2
US 6,858,738 · App. 10/431,536 · Granted Feb 22, 2005

Process for making amlodipine, derivatives thereof, and precursors therefor

Assignee: Synthon BV
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Quick Facts
Patent No.
US 6,858,738
App. No.
10/431,536
Granted
Feb 22, 2005
Kind
B2
Abstract

Amlodipine and related analogues thereof are prepared by the following general reaction scheme: R 1 and R 2 each independently represent a C 1 -C 4 alkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.

Claims (9)

1. A compound having the formula (3):

wherein R 2 is a C 1 -C 4 alkyl group.

2. The compound according to claim 1 , wherein said compound is in isolated form.

3. The compound according to claim 1 in the form of an oil.

4. The compound according to claim 1 , wherein said compound is in the form of a mixture of cis and trans isomers.

5. The compound according to claim 1 , wherein R 2 is a methyl group, an ethyl group, or an isopropyl group.

6. The compound according to claim 4 , wherein R 2 is an ethyl group.

7. The compound according to claim 5 , wherein said compound is in the form of a mixture of cis and trans isomers.

8. The compound according to claim 5 , in the form of an oil.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 18, 2005
From: SYNTHON BV
To: SYNTHON IP INC.
Reel/Frame 016026/0687 →
Continuity (4)
Division 0993884000 · Aug 27, 2001
Continuation In Part 0980935100 · Mar 16, 2001
Provisional Application 6025861300 · Dec 29, 2000
Related Publication 20030220501A1 · Nov 27, 2003