Crystalline Fosaprepitant Dicyclohexylamine Salt And Its Preparation
AssigneeNavinta LLC
InventorsJigneshkumar Jasubhai Patel, Raja Jeyakumar John Muthiah
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Abstract
The present invention provides dicyclohexylamine salt of fosaprepitant (fosaprepitant DCHA), a process for preparing fosaprepitant DCHA, and a use of fosaprepitant DCHA in the preparation of pharmaceutically acceptable fosaprepitant dimeglumine with high purity. Fosaprepitant dimeglumine is prepared by treating fosaprepitant DCHA with an acid to form fosaprepitant, followed by adding N-methyl-D-glucamine to fosaprepitant.
Claims20
A fosaprepitant di(dicyclohexylamine) salt of formula II:
A process for preparing a fosaprepitant di(dicylohexylamine) salt of formula II comprising:
- (1) hydrogenating a dibenzyl fosaprepitant of formula IV in the presence of a mixture comprising 10% Pd/C, dicyclohexylamine, and a solvent system to form the fosaprepitant di(dicylohexylamine) salt of formula and
- (2) isolating the fosaprepitant di(dicylohexylamine) salt of formula II.
A process for the preparation of fosaprepitant di(N-methyl-D-glucamine) salt of formula Ia:
- comprising:
- (1) treating a solution of fosaprepitant di(dicyclohexylamine) salt of formula II with an acid to obtain fosaprepitant of formula I;
- (2) dissolving fosaprepitant of formula I and N-methyl-D-glucamine in a solvent to obtain a solution of fosaprepitant di(N-methyl-D-glucamine) salt of formula Ia;
- and
- (3) isolating fosaprepitant di(N-methyl-D-glucamine) salt of formula Ia.
Dependencies are inferred from the claim text.