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US 10,479,769 B2Granted
Processes for the preparation of eluxadoline
AssigneeSun Pharmaceutical Industries Limited
InventorsMurad Ismail Inamdar, Sriram Hari Mohan, Ketan Vithalbhai Hirpara
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Abstract
The present invention relates to processes for the preparation of eluxadoline. The present invention also provides a compound of Formula V, a process for its preparation, and its use for the preparation of eluxadoline.
Claims10
A process for the preparation of eluxadoline of Formula I,
- comprising
- a) deprotecting a compound of Formula II
- wherein PG is a nitrogen protecting group;
- in the presence of a deprotecting agent to obtain a compound of Formula III;
- b) reductive amination of the compound of Formula III with a compound of Formula IV
- wherein R is hydrogen or C1-6 alkyl;
- followed by the treatment with an acid to obtain a compound of Formula V
- wherein R is hydrogen or C1-6 alkyl;
- and
- c) converting the compound of Formula V to eluxadoline of Formula I.
7 more elements
A compound of Formula V,
- wherein the salt is selected from the group consisting of citrate, acetate, fumarate, lactate, maleate, malate, tartrate, benzoate, mesylate, oxalate, tosylate, and succinate;
- and
- wherein R is hydrogen or C1-6 alkyl.
A compound of Formula Va,
- wherein the salt is selected from the group consisting of citrate, acetate, fumarate, lactate, maleate, malate, tartrate, benzoate, mesylate, oxalate, tosylate, and succinate.
Dependencies are inferred from the claim text.