Title:
A PROCESS FOR THE PREPARATION OF ASENAPINE AND NOVEL SALTS THEREOF
Document Type and Number:
WIPO Patent Application WO/2013/024492
Kind Code:
A3
Abstract:
A process for preparation of asenapine of formula (1) or its acid addition salts; The said process comprises preparation of trans racemate of asenapine by reacting trans- 1 1-chloro-2,3,3a, 12b-tetrahydro-2-methyl-lH-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-l-one with mixture of aluminium chloride and lithium aluminium hydride in solvent followed by converting it into acid addition salt of asenapine followed by hydrolyzing the acid addition salt into trans racemate asenapine base and converting the asenapine base into acid addition salt. Asenapine sulphate of formula (Via) and asenapine maleate of formula (IVb) are also disclosed. The co-precipitate of acid addition salt of asenapine with a pharmaceutically acceptable excipient of formula (V); is also disclosed.
Inventors:
MATHAD VIJAYAVITTHAL THIPPANNACHAR (IN)
SOLANKI PAVANKUMAR VRAJLAL (IN)
UPPELLI SEKHAR BABU (IN)
CHAVAN SHRAVAN RATAN (IN)
SOLANKI PAVANKUMAR VRAJLAL (IN)
UPPELLI SEKHAR BABU (IN)
CHAVAN SHRAVAN RATAN (IN)
Application Number:
PCT/IN2012/000463
Publication Date:
May 23, 2013
Filing Date:
June 29, 2012
Export Citation:
Assignee:
MEGAFINE PHARMA P LTD (IN)
MATHAD VIJAYAVITTHAL THIPPANNACHAR (IN)
SOLANKI PAVANKUMAR VRAJLAL (IN)
UPPELLI SEKHAR BABU (IN)
CHAVAN SHRAVAN RATAN (IN)
MATHAD VIJAYAVITTHAL THIPPANNACHAR (IN)
SOLANKI PAVANKUMAR VRAJLAL (IN)
UPPELLI SEKHAR BABU (IN)
CHAVAN SHRAVAN RATAN (IN)
International Classes:
C07D491/044; A61K31/407; A61P25/18
Domestic Patent References:
| WO2006106136A1 | 2006-10-12 |
Foreign References:
| US20080009619A1 | 2008-01-10 |
Other References:
KEVIN K-C LIU ET AL: "Synthetic approaches to the 2009 new drugs", BIOORGANIC & MEDICINAL CHEMISTRY, PERGAMON, GB, vol. 19, no. 3, 16 December 2010 (2010-12-16), pages 1136 - 1154, XP028133979, ISSN: 0968-0896, [retrieved on 20101224], DOI: 10.1016/J.BMC.2010.12.038
Attorney, Agent or Firm:
SHILPA, Gharve (C-302 RNA Regency Park,M.G. Road, Kandivali ,Mumbai - 7, Maharashtra, IN)
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