The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Oct. 09, 2012

Filed:

Aug. 31, 2009
Applicants:

Vijayvitthal Thippannachar Mathad, Maharashtra, IN;

Navnath Chintaman Niphade, Maharashtra, IN;

Anil Chaturlal Mali, Maharashtra, IN;

Kunal Madhav Jagtap, Maharashtra, IN;

Bhushan Sudhakar Pandit, Maharashtra, IN;

P. Raghvendra Kumar, Maharashtra, IN;

Shashikant Baburao Landge, Nashik, IN;

Inventors:

Vijayvitthal Thippannachar Mathad, Maharashtra, IN;

Navnath Chintaman Niphade, Maharashtra, IN;

Anil Chaturlal Mali, Maharashtra, IN;

Kunal Madhav Jagtap, Maharashtra, IN;

Bhushan Sudhakar Pandit, Maharashtra, IN;

P. Raghvendra Kumar, Maharashtra, IN;

Shashikant Baburao Landge, Nashik, IN;

Assignee:

Megafine Pharma(P) Ltd., Mumbai, Maharashtra, IN;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07D 453/04 (2006.01); A61K 31/44 (2006.01);
U.S. Cl.
CPC ...
Abstract

A method for the preparation of solifenacin by reacting quinuclidin-3-ol and bis (aryl) carbonate to form (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa); and treating (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa) with (1S)-1-phenyl- 1,2,3,4-tetrahydroisoquinoline of formula (V) in an inert atmosphere to form a Solifenacin base, which is converted into its pharmaceutically acceptable salts. The invention also provides a compound, (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa), which is used as an intermediate for the preparation of Solifenacin base and a process for the preparation thereof.


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