Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2005-03-04
2009-12-08
Morris, Patricia L (Department: 1625)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
active
07629465
ABSTRACT:
An improved process for the manufacture of Clopidogrel starting from 2-(2-thienyl) ethylamine, which eliminates the isolation of an unstable intermediate like 2-(2-thienyl) ethyl formimine by subjecting it to a one pot cyclization to get 4, 5, 6, 7-tetrahydrothieno (3,2-c) pyridine of Formula II and further reacting with halo-compound of Formula III (where X is Cl or Br) at 20 to 90° C. temperature characterized in a solvent like water and/or dichloroethane in presence of organic or inorganic bases is disclosed herein. This invention further discloses a process for resolution of racemic Clopidogrel into its optical antipodes and converting the dextroclopidogrel base into its known polymorphs namely ‘Form I’ or ‘Form II’ in solvents selected from methyl propyl ketone, methyl isopropyl ketone, diethyl ketone or their mixture thereof, mixture of ethyl acetate and methyl propyl ketone, mixture of ethyl acetate and methyl isopropyl ketone, or mixture of ethyl acetate and diethyl ketone or ethyl acetate.
REFERENCES:
patent: 6635763 (2003-10-01), Pandey et al.
patent: 6767913 (2004-07-01), Lifshitz et al.
Bernstein “Polymorphism in moleciar crystals” Oxford:Clarendon Press 115-118,272 (2002).
Barve Sanjay Govind
Bhayani Priti Jayesh
Burudkar Sandeep Madhavrao
Kumar Ashok
Kushwaha Lavkesh Dayashankar
Blank Rome LLP
IPCA Laboratories Ltd.
Morris Patricia L
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