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

J. Harnett, Gerard; Hauck, Ulrike; J. Hayes, John; Hoffmann, Ursula; Lohri, Bruno; Meade, Michael; Morawitz, Falk; P. Plesniak, Mateusz; Stahr, Helmut; E. Veits, Joachim; Walsh, Andrew; Zogg, Andreas; Reents, Reinhard; A. Smith, Dennis; E. Martin, Rainer

doi:10.1021/acs.oprd.3c00304

Public

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

Published in Organic Process Research & Development • Nov 13, 2023

Authors:

Gerard J. Harnett

Ulrike Hauck

John J. Hayes

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 des...

Subject

Alkylation

Chemistry

Nitrile

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