Emcure Pharmaceuticals Limited

Golakchandra Sudarshan Maikap

Mukund Keshav Gurjar

Samit Satish Mehta

Narendra Kumar Tripathy

Swapnil Panditrao Sonawane

Rajendra Dagesing Mahale

Sanjay Shankar Pawar

Pankaj Shalikrao

Shivnath Bhaupatil Shinde

Gulabrao Dagadu Patil

Vijay Keshav Kalhapure

Ashok Tukaram Chaudhari

Tushar Pandurang Khaladkar

Shashikant Gangaram Joshi

Mangesh Gorakhanath Kamble

Sachin Aravind Badhe

Pankaj Shalikrao Patil

Devising Rameshsing Pardeshi

The present invention relates to the preparation of stable pyridone disulphide derivatives having general formula (I) and its stereoisomers, which are useful in the treatment of gastrointestinal disorders. Pyridone disulphide derivatives (I) wherein, R, Rand Rare independently alkyl, alkoxy, halogen, halogenated alkoxy, halogenated alkyl, hydrogen and could be the same or different and X is CH or N. Ris methyl, methoxy, fluorine, trifluoromethyl, difluoromethoxy and hydrogen, Ris methyl, methoxy and hydrogen, and Ris methyl and hydrogen.

Pyridone derivatives as acid secretion inhibitors and process for preparation thereof

The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).

Synthesis of Raltegravir

Synthesis of raltegravir

Disclosed is process for the preparation of a key Rilpivirine intermediate namely, (E)-4-(2-cyanoethenyl)-2,6-dimethylphenylamine hydrochloride (II) by a process comprising reaction of the tetrafluoroborate salt of the diazonium ion of 2,6-dimethyl-4-amino-1-carboxybenzyl phenylamine (VI) with acrylonitrile in presence of palladium acetate, followed by treatment with an acid and its subsequent conversion to the hydrochloride salt (II), wherein the undesired Z isomer is less than 0.5% and provides Rilpivirine hydrochloride having Z isomer less than 0.1%.

Rilpivirine process

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Pune, India

Golakchandra Sudarshan Maikap