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1. WO2012159992 - PROCESS FOR OBTAINING RIVAROXABAN AND INTERMEDIATE THEREOF

Publication Number WO/2012/159992
Publication Date 29.11.2012
International Application No. PCT/EP2012/059272
International Filing Date 18.05.2012
Chapter 2 Demand Filed 17.01.2013
IPC
C07D 413/10 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
C07D 413/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
CPC
A61K 31/5377
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
C07D 413/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
C07D 413/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
Applicants
  • INTERQUIM, S.A. [ES]/[ES] (AllExceptUS)
  • BERZOSA RODRÍGUEZ, Xavier [ES]/[ES] (UsOnly)
  • MARQUILLAS OLONDRIZ, Francisco [ES]/[ES] (UsOnly)
  • LLEBARIA SOLDEVILLA, Amadeo [ES]/[ES] (UsOnly)
  • SERRA COMAS, Carme [ES]/[ES] (UsOnly)
Inventors
  • BERZOSA RODRÍGUEZ, Xavier
  • MARQUILLAS OLONDRIZ, Francisco
  • LLEBARIA SOLDEVILLA, Amadeo
  • SERRA COMAS, Carme
Agents
  • ZBM Patents- Zea, Barlocci & Markvardsen
Priority Data
P 20113081720.05.2011ES
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR OBTAINING RIVAROXABAN AND INTERMEDIATE THEREOF
(FR) PROCÉDÉ PERMETTANT D'OBTENIR DU RIVAROXABAN ET INTERMÉDIAIRE DE CELUI-CI
Abstract
(EN) This invention relates to a procedure for obtaining a thiophene-2-carboxamide compound, specifically rivaroxaban, which comprises the (i) fragmentation of the N=C bond of a compound of formula 23 where R1 is selected among hydrogen, halogen, and (C1-C6)alkyl; and (ii) acylation of the resulting intermediate with 5-chloro-tiofen-2-carbonyl chloride in a solvent medium, in the presence of a base. The invention also relates to the compounds of formula 23 and their use in the obtention of rivaroxaban.
(FR) Cette invention porte sur un mode opératoire permettant d'obtenir un compose thiophène-2-carboxamide, précisément du rivaroxaban, qui comprend (i) la rupture de la liaison N=C d'un composé de formule 23 dans laquelle R1 est choisi parmi un atome d'hydrogène, un atome d'halogène et un groupe alkyle en C1-C6 ; et (ii) l'acylation de l'intermédiaire ainsi obtenu avec du chlorure de 5-chlorothiophène-2-carbonyle dans un milieu solvant, en présence d'une base. L'invention porte également sur les composés de formule 23 et sur leur utilisation dans l'obtention de rivaroxaban.
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