Process for making modulators of cystic fibrosis transmembrane conductance regulator
AssigneeVertex Pharmaceuticals Incorporated
InventorsJohn DeMattei, Adam R. Looker, Bobbianna J. Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
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Abstract
The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.
Claims14
1-58. (canceled)
A process for the preparation of a compound of Formula 8
- comprising nitrating a compound of Formula 7 using a mixture of sulfuric acid and nitric acid in the presence of dichloromethane
- wherein PG is a protecting group and R2 and R4 are each tert-butyl, and wherein the nitro compound of Formula 8 is purified by crystallization.
A process for the preparation of Compound 31, comprising contacting Compound 30 with a mixture of nitric acid and sulfuric acid in the presence of dichloromethane
Dependencies are inferred from the claim text.