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US 12,024,491 B2Granted
Processes for making modulators of cystic fibrosis transmembrane conductance regulator
AssigneeVertex Pharmaceuticals Incorporated
InventorsBerenice Lemercier Lewandowski, Robert Lewis, Adam Looker, Adam Morgan, Stefanie Roeper, Michael Ryan, Juan Gabriel Solsona Rocabert, Nathan Wilde
Life of this patent
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Abstract
The disclosure provides processes for synthesizing compounds for use as CFTR modulators.
Claims21
A process for the preparation of compound 2:
- comprising:
- a) converting compound 21:
- into compound 20:
- wherein the conversion of compound 21 into compound 20 is performed in the presence of KNO3 and/or NaNO3, AlCl3, and optionally one or more of trimethylsilyl chloride and TiCl4;
- b) converting compound 20 into compound 7:
- c) reacting compound 3:
- with compound 7 to produce compound 8:
- (d) converting compound 8 into compound 2;
- wherein the methyl (Me) of the —OCO2Me of compound 7, 8, 20, and 21 is optionally replaced by a group selected from aliphatic, heteroaliphatic, heterocyclic, haloaliphatic, aryl, and heteroaryl.
6 more elements
A process for the preparation of compound 2:
- comprising:
- a) converting compound 16:
- into compound 15:
- wherein the conversion of compound 16 into compound 15 is performed in the presence of KNO3 and/or NaNO3, AlCl3, and optionally one or more of trimethylsilyl chloride and TiCl4;
- b) converting compound 15 into compound 7:
- c) reacting compound 3:
- with compound 7 to produce compound 8:
- (d) converting compound 8 into compound 2;
- wherein the methyl (Me) of the —OCO2Me of compounds 7, 8, 15, and 16 is optionally replaced by a group selected from aliphatic, heteroaliphatic, heterocyclic, haloaliphatic, aryl, and heteroaryl.
6 more elements
Dependencies are inferred from the claim text.