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Forster Reaction Delivers Generic Drug

A novel synthetic route to make a hyperparathyroidism drug uses a century-old, unexplored method

by Celia Henry Arnaud
March 14, 2011 | A version of this story appeared in Volume 89, Issue 11

Indian researchers have devised a novel synthetic route to Amgen’s hyperparathyroidism drug cinacalcet hydrochloride for the generic drug market by using the Forster reaction, a century-old unexplored method to make secondary amines (Org. Process Res. Dev., DOI: 10.1021/op200016a). When it comes to producing a generic drug, pharmaceutical companies first pick a potential target that will provide them with a competitive advantage and then devise a low-cost synthesis and purification route that doesn’t infringe on existing patents, explains Vijayavitthal T. Mathad of Megafine Pharma, who led the research team. “It’s essential to find white space in which to operate,” Mathad says, “which often means devising a completely new route.” After conducting a retrosynthetic analysis of cinacalcet, Mathad and coworkers settled on the Forster reaction, a condensation of an amine with an aldehyde followed by addition of an alkyl halide and hydrolysis, which was first described in 1899 by British chemist Martin O. Forster (J. Chem. Soc. Trans., DOI: 10.1039/CT8997500934). The researchers are using it in a one-pot reaction scaled up to 10-kg batches of cinacalcet, which they believe is the first industrial application of the Forster reaction.


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