Hikal Limited

Arulselvan Mariadas

Nagarajan Kuppuswamy

Sivaramakrishnan Hariharan

This invention relates to an improved process for the preparation of amino methyl cyclo alkane acetic acids. This invention particularly relates to an improved process for the preparation of gabapentin (which is chemically known as 1-aminomethyl-1-cyclohexaneacetic acid), which is a very well known agent useful for the treatment of epilepsy and other cerebral disorders. In the chemical series of 1-amino methyl cyclo alkane-1-acetic acids, Gabapentin, which is 1-amino methyl cyclo hexane-1-acetic acid has been developed as a drug having anti convulsive properties.

Process for the preparation of amino methyl cyclo alkane acetic acids

The present invention provides an improved process for the preparation of gabalactam of formula 1 that includes preparing an aqueous solution of an alkali or alkaline earth metal hydroxide, adding bromine to the resulting solution to give an appropriate alkali or alkaline earth metal hypobromite; adding an amide of the formula 4 aging the resultant mixture; heating the mixture to a temperature in a range of 80 to 100 degrees C.; extracting with nonpolar solvent and distilling under reduced pressure to obtain gabalactam.

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Bengaluru, India

Arulselvan Mariadas