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US 11,708,331 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.
Claims9
A compound selected from:
- and salts thereof.
A process for the preparation of compound 1:
- comprising:
- a) converting compound 12:
- into compound 11A:
- wherein the conversion of compound 12 into compound 11A is performed in the presence of KNO3 and/or NaNO3, AlCl3, and optionally one or more of trimethylsilyl chloride and TiCl4;
- b) converting compound 11A into compound 4:
- c) reacting compound 3:
- with compound 4 to produce compound 5:
- and
- d) converting compound 5 into compound 1;
- wherein the methyl (Me) of the —OCO2Me of each of compounds 4, 5, 11A, and 12 is optionally replaced by a group selected from aliphatic, heteroaliphatic, heterocyclic, haloaliphatic, aryl, and heteroaryl.
7 more elements
A process for the preparation of compound 11A:
- comprising converting compound 12:
- into compound 11A;
- wherein the conversion of compound 12 into compound 11A is performed in the presence of KNO3 and/or NaNO3, AlCl3, and optionally one or more of trimethylsilyl chloride and TiCl4;
- and
- wherein the methyl (Me) of the —OCO2Me of each of compounds 11A and 12 is optionally replaced by a group selected from aliphatic, heteroaliphatic, heterocyclic, haloaliphatic, aryl, and heteroaryl.
2 more elements
Dependencies are inferred from the claim text.