Process for making modulators of cystic fibrosis transmembrane conductance regulator
AssigneeVertex Pharmaceuticals Incorporated
InventorsJohn Demattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D. J. Grootenhuis, Fredrick F. Van Goor, Martyn C. 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.
Claims3
A process for the preparation of a compound of Formula 1,
- or a pharmaceutically acceptable salt thereof, comprising:
- (a) coupling a carboxylic acid of Formula 2,
- or a pharmaceutically acceptable salt thereof, with an aniline of Formula 3,
- or a pharmaceutically acceptable salt thereof, in the presence of a coupling agent under conditions sufficient to produce a compound of Formula 4,
- or a pharmaceutically acceptable salt thereof;
- and
- (b) cleaving the methoxy formyl protecting group from the phenolic oxygen atom of Formula 4 under conditions sufficient to yield a compound of Formula 1, or a pharmaceutically acceptable salt thereof.
A compound of Formula 3, or a pharmaceutically acceptable salt thereof.
A compound of Formula 4, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.