# US 2013/0158270 A1 · Process for the manufacture of dabigatran etexilate

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- Number: US 2013/0158270 A1
- Document ID: US20130158270A1
- Status: Published application
- Kind: A1
- Application number: 13/768,350
- Filed: 2013-02-15
- Published: 2013-06-20
- Earliest claimed: 2009-11-18
- Assignees: Boehringer Ingelheim International GmbH
- Inventors: Frieder GNAD; Stefan SCHMITT; Hermann MUELLER-BOETTICHER; Helmut HEITGER; Seigfried MEINECK; Rolf DACH; Ingo HEDDESHEIMER
- Web page: https://patentgrep.com/patent/US20130158270A1

## CPC

- C07D 401/12: linked by a chain containing hetero atoms as chain links
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 9/06: Antiarrhythmics
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 271/64: Y being a hydrogen or a carbon atom, e.g. benzoylcarbamates
- C07C 303/32: of salts of sulfonic acids
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

An improved process for preparing dabigatran etexilate, as well as analogous compounds of formula 7, is described.

## Claims

### Claim at position 1

1-10. (canceled)

### Claim 11

A compound of formula 7,
prepared by a process comprising the step of reacting a compound of formula 6
with a compound of formula 3
wherein in compounds 7, 6 and 3, R1, R2 and R3 each independently of one another denote C1-6-alkyl or halogen (Hal), and wherein Hal is chlorine or bromine

### Claim 12

Compound of formula 8,
prepared by a process comprising the step of reacting a compound of formula 6
with a compound of formula 3
wherein in compounds 7, 6 and 3, R1, R2 and R3 each independently of one another denote C1-6-alkyl or halogen (Hal), and wherein Hal is chlorine or bromine, and wherein the compound 7 is reacted with methanesulphonic acid 9 to form a compound of formula 8.

### Claim 13

A compound of formula 3
wherein the group R1 denotes C1-6-alkyl.

### Claim 14 (depends on 13)

The compound according to claim 13, wherein R1 is n-hexyl.

### Claim 15

A compound of formula 6
wherein the groups R2 and R3 each independently of one another denote C1-6-alkyl or halogen (Hal), and wherein Hal is chlorine or bromine.

### Claim 16 (depends on 15)

The compound according to claim 15, wherein R2 is methyl, R3 is ethyl and Hal is chlorine.