Title of Invention

AN IMPROVED PROCESS FOR THE PREPARATION OF MONTELUKAST AND ITS AMINE SALTS

Abstract The present invention provides an improved process for the preparation of [R- (E)-I- [[[I-[3-[2-[7-chloro-2-quinolinyl] ethenyl] phenyl]-3-[2-(I-hydroxy-I-methylethyl) phenyl] propyl] thio] methyl] cyclopropaneacetic acid (Montelukast) of Formula (1) and its amine salts comprising of primary, secondary and tertiary amines. The amine salts of Montelukast are precursor for the preparation of Montelukast sodium. The improved process for the preparation comprises, mesylation of 2-(2-(3(S)-(3-(2-(7-chloro-2- quinolinyl) ethenyl) phenyl)-3-hydroxypropyl) phenyl)-2-propanol of Formula (2) with methane sulfonyl chloride using triethyl amine as a base, the resulted mesylated compound of Formula (3) is condensed with I-(mercaptomethyl) cyclopropane aceticacid of Formula (4) in the presence of simple base such as sodium hydroxide and sodium methoxide in a solvent to afford the Montelukast. The Montelukast is further converted into its amine salts in a conventional methods. The process for the preparation of Montelukast and its amine salts of the present invention is simple, cost-effective and environment friendly.
Full Text

Documents:

505-mas-2002 abstract.pdf

505-mas-2002 claims.pdf

505-mas-2002 correspondence others.pdf

505-mas-2002 correspondence po.pdf

505-mas-2002 description (complete).pdf

505-mas-2002 form 1.pdf

505-mas-2002 form 18.pdf


Patent Number 236239
Indian Patent Application Number 505/MAS/2002
PG Journal Number 42/2009
Publication Date 16-Oct-2009
Grant Date 12-Oct-2009
Date of Filing 05-Jul-2002
Name of Patentee DR REDDY'S LABORATORIES
Applicant Address 7-1-27, ameerpet HYDERABAD-500016.
Inventors:
# Inventor's Name Inventor's Address
1 BUCHI REDDY REGURI 404, BALAJI RESIDENCY, 88/A MIGH, VENGAL RAO NAGAR, HYDERABAD-500038.
2 SATYANARAYANA BOLLIKONDA H.NO. 5-172 DEEPTHISRI NAGAR CHANDANAGAR, HYDERABAD-500050.
3 VEERA VENKATA NAGA CHANDRA SEKHAR BULUSU PLOT NO.19, GMSD COLONY, VIVEKANANDA NAGAR, KUKATPALLY, HYDERABAD-500072.
PCT International Classification Number C07D215/00
PCT International Application Number N/A
PCT International Filing date
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 NA