Title:
SALT OF, AND PROCESSES FOR THE PREPARATION OF, 1-ISOPROPYL-4-{[4-(TETRAHYDRO-2H-PYRAN- 4-YLOXY)PHENYL]CARBONYL}HEXAHYDRO-1H-1,4-DIAZEPINE
Document Type and Number:
WIPO Patent Application WO/2010/018231
Kind Code:
A3
Abstract:
The invention relates to 1-isopropyl-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}hexahydro-1H-1,4-diazepine mono-maleate, and crystalline Form 1 thereof. The invention also provides a process for the preparation of 1-isopropyl-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}hexahydro-1H-1,4-diazepine (Formula (A)) or a pharmaceutically acceptable salt thereof, which process comprises: (a) reacting a non-acid-chloride derivative of 4-(tetrahydro-2H-pyran-4-yloxy)benzoic acid, in which the carboxylic acid group has been activated, with 1-isopropyl-hexahydro-1H-1,4-diazepine; and (b) optionally preparing a pharmaceutically acceptable salt of 1-isopropyl-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}hexahydro-1H-1,4-diazepine. Process (a) typically comprises activation of 4-(tetrahydro-2H-pyran-4-yloxy)benzoic acid with a coupling reagent, preferably carbonyl diimidazole, followed by reaction with 1-isopropyl-hexahydro-1H-1,4-diazepine. The invention also provides 1-isopropyl-hexahydro-1H-1,4-diazepine bis-trifluoroacetate. The invention also provides a process for preparing a compound of formula (III) wherein P represents a protecting group.
Inventors:
DAY CAROLINE JANE (GB)
KEEL TREVOR RAYMOND (GB)
RASSIAS GERACIMOS (GB)
KEEL TREVOR RAYMOND (GB)
RASSIAS GERACIMOS (GB)
Application Number:
PCT/EP2009/060578
Publication Date:
April 08, 2010
Filing Date:
August 14, 2009
Export Citation:
Assignee:
GLAXO GROUP LTD (GB)
DAY CAROLINE JANE (GB)
KEEL TREVOR RAYMOND (GB)
RASSIAS GERACIMOS (GB)
DAY CAROLINE JANE (GB)
KEEL TREVOR RAYMOND (GB)
RASSIAS GERACIMOS (GB)
International Classes:
C07D405/12; A61K31/5513; A61P25/28
Domestic Patent References:
| WO2005040144A1 | 2005-05-06 | |||
| WO2009030716A1 | 2009-03-12 |
Attorney, Agent or Firm:
BREEN, Anthony Paul et al. (Corporate Intellectual Property CN925.1980 Great West Road, Brentford Middlesex TW8 9GS, GB)
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