Amneal Pharmaceuticals LLC

Megafine Pharma (p) Ltd.

Vijayavitthal Thippannachar Mathad

Navnath Chintaman Niphade

Gorakshanath Balasaheb Shinde

Sharad Subhash Ippar

Shrikant Prataprao Deshmukh

Raghavendra Kumar Panchangam

Kunal Madhav Jagtap

Chandrashekar Trimbak Gaikwad

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 Cinacalcet is disclosed comprising treating (R)-1-naphthyl ethylamine with an aromatic aldehyde to form (1R)-1-(2-naphthyl)-N-(aryl methylene)ethanamine derivative of Formula (IV), which is further treated with 1-(3-halopropyl)-3-(trifluoromethyl)benzene of Formula (V) to obtain an iminium salt of Formula (VI), followed by hydrolysis to obtain Cinacalcet free base.

Method for the preparation of cinacalcet and intermediates and impurities thereof

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Vijayavitthal Thippannachar Mathad