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US 2014/0155614 A1Published application
Pharmaceutical intermediates and process for the preparation thereof
AssigneeEgis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
InventorsImre Kiraly, Tibor Szabo, Gyula Simig, Balazs Volk, Laszlo Szlavik, Jozsef Barkoczy, Gyorgy Ruzsics, Gyula Lukacs, Laszlo Pongo, Andras Boza, Maria Tothne Lauritz, Maria Kovacs
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Abstract
The present invention relates to a process for the preparation of dabigatran etexilate of the formula or pharmaceutically accepted salts thereof.
Claims17
Process for the preparation of dabigatran etexilate of the Formula
- or pharmaceutically acceptable salts thereof
- which comprises reducing a compound of the general Formula
- wherein
- R stands for hydrogen;
- C1-6 straight or branched chain, saturated or partially or completely un-saturated hydrocarbon chain,
- C1-6 straight or branched chain, partially or completely halogenated alkyl;
- aryl or
- methoxymethyl
- optionally converting the compound of the Formula
- thus obtained into a salt and
- reacting the compound of the Formula (2) or a salt thereof with chloro hexyl formate to yield the compound of the Formula (1) and
- optionally forming a salt from the compound of the Formula (1).
9 more elements
4-15. (canceled)
A product, which is
- the 1:2 p-toluenesulfonic acid salt of ethyl-N-[(2-{[(4-carbamimidoylphenyl)-amino]-methyl}-1-methyl-1H-benzimidazole-5-yl)-carbonyl]-N-pyridine-2-yl-β-alaninate (2);
- or
- the 1:2 acetic acid salt of ethyl-N-[(2-{[(4-carbamimidoylphenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-yl)-carbonyl]-N-pyridine-2-yl-β-alaninate (2);
- or
- a compound of the general Formula (15)
- wherein
- R stands for hydrogen;
- C1-6 straight or branched chain, saturated or partially or completely un-saturated hydrocarbon chain,
- C1-6 straight or branched chain, partially or completely halogenated alkyl;
- aryl or
- methoxymethyl
- or a salt thereof;
- or
- the monooxalate salt of a compound of the general Formula (15)
- wherein
- R is methyl;
- or
- a compound of the general Formula (14)
- wherein
- R stands for hydrogen;
- C1-6 straight or branched chain, saturated or partially or completely un-saturated hydrocarbon chain,
- C1-6 straight or branched chain, partially or completely halogenated alkyl;
- aryl or
- methoxymethyl,
- or a salt thereof;
- or
- a compound of the general Formula (13)
- wherein
- R stands for hydrogen;
- C1-6 straight or branched chain, saturated or partially or completely un-saturated hydrocarbon chain,
- C1-6 straight or branched chain, partially or completely halogenated alkyl;
- aryl or
- methoxymethyl,
- R″ stands for
- C1-6 straight or branched chain, saturated or partially or completely un-saturated hydrocarbon chain,
- C1-6 straight or branched chain, partially or completely halogenated alkyl or
- aralkyl,
- or a salt thereof.
35 more elements
Dependencies are inferred from the claim text.