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(12) PATENT APPLICATION PUBLICATION
(19) INDIA (21) Application No.: 1197/MUM/2004 A
(22) Date of filing of Application: 05/11/2004 (43) Publication Date: 09/06/2006
(54) Title of the invention: INDUSTRIAL PROCESS FOR THE PREPARATION OF
TOLTERODINE TARTRATE
(51) International classification : C07C 215/54,
C07D 311/00
(31) Priority Document No : NIL
(32) Priority Date : NIL
(33) Name of priority country : NIL
(86) International Application No : NIL
and Filing Date : NIL
(87) International Publication No : NIL
(61) Patent of addition to :
Application No
NIL
(62)
Filed on : N.A.
Divisional to Application No : NIL
Filed on : N.A.
(71) Name of Applicant:
LUPIN LIMITED
Address of the Applicant:
159, CST ROAD, KALINA,
SANTACRUZ (EAST), MUMBAI-
400098, MAHARASHTRA, INDIA.
(72) Name of the Inventor:
1. BHANU MANJUNATH
NARAYAN
2. JAIN MURLIDHAR AJINATH
3. TEMBHURNIKAR WAMAN
KARTIK
Filed U/S 5(2) before The Patents
(Amendment) Act, 2005: NO
(57) Abstract: A process for the preparation of tolterodine tartrate of formula (I), which comprises converting the
lactone of formula (II) to the compound of formula (IIa) by treating with sodium borohydride in a alcoholic
solvent such as isopropyl alcohol, methylating the phenolic group in compound of formula (IIa) using dimethyl
sulphate under basic conditions to get compound of formula (IV), tosylating the alcohol of formula (IV) in
presence of an organic base such as triethyl amine, condensing the tosyl derivative of formula (V) with
diisoproylamine in a suitable organic solvent such as acetonitrile to get the amine compound of formula (VI),
deprotecting the phenoilc group of compound of formula (VI) using aqueous solution of hydrobromic acid,
liberating the free base tolterodine from the hydrobromide salt, by treating with a inorganic base such as ammonia,
resolving the racemic tolterodine obtsained in step-vi, by treating with L-tartaric acid in an alcoholic solution, and
purifying L-tolterodine tartrate from a methanolic solution.
Drawing Sheets: NIL
Total Pages: 30.
Fig. Nil
The Patent Office Journal 09/06/2006 10883