Development and Demonstration of a High-Volume Manufacturing Process for a Key Intermediate of Dalcetrapib: Investigations on the Alkylation of Carboxylic Acids, Esters, and Nitriles
Gerard J. Harnett,
Ulrike Hauck,
John J. Hayes
et al.
Abstract:Dalcetrapib (1), a cholesterol ester transfer protein inhibitor, was a clinical candidate at Roche until 2012. By this time, manufacturing processes capable of efficiently delivering kilotonne annual volumes of Dalcetrapib had been developed and demonstrated at the commercial scale. This paper describes the development of synthetic routes for the manufacture of key intermediate 1-(2-ethylbutyl)-cyclohexanecarboxylic acid (2) and selection of the preferred process. The selected process involves novel methods fo… Show more
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