Megafine Pharma (p) Ltd.

Kunal Madhav Jagtap

Navnath Chintaman Niphade

Bhushan Sudhakar Pandit

Vijayavitthal Thippannachar Mathad

Chandrashekar Trimbak Gaikwad

Vijayvitthal Thippannachar Mathad

Anil Chaturlal Mali

P Raghvendra Kumar

Shashikant Baburao Landge

Mathad Vijayavitthal Thippannachar Thippannachar

A novel ammonium salt of Bosentan of formula (VIII); has been disclosed. The salt may be either crystalline or amorphous or mixture of Crystalline and amorphous form. A novel single pot process for the preparations of ammonium salt of Bosentan has been disclosed. The process comprises reacting the 4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine with 4-tert-butylbenzenesulfonamide in the presence of solvent and a base; adding ethylene glycol to the reaction mass and isolating the ammonium salt of Bosentan. The ammonium salt of Bosentan is converted into Bosentan and further into Bosentan Monohydrate which are substantially free from dimer impurity and 6-hydroxy impurity. 

Process for preparation of bosentan

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.

Method for the preparation of solifenacin and intermediate thereof

Growing community of inventors

Maharashtra, India

Kunal Madhav Jagtap