Back to results
US 2017/0291874 A1Published application
Process for the Manufacture of Idalopirdine via Hydrogenation of an Imine
AssigneeH. Lundbeck A/S
InventorsMikkel Fog Jacobsen, Florian Anton Martin Huber
Life of this patent
Estimating the term…
Abstract
The present invention relates to the preparation of N-(2-(6-fluoro-1H-indol-3-yl)-ethyl)-3-(2,2,3,3-tetrafluoropropoxy)-benzylamine (Compound I), INN-name idalopirdine, and pharmaceutically acceptable salts thereof:
Claims18
A process for the preparation of N-(2-(6-fluoro-1H-indol-3-yl)-ethyl)-3-(2,2,3,3 tetrafluoropropoxy)-benzylamine (Compound (I)), and pharmaceutically acceptable salts thereof, comprising the steps of:
- 1) forming a reaction mixture that comprises Compound (V) from Compound (III) and Compound (IV) in a solvent or solvent mixture with or without removal of water, and
- 2) reacting the Compound (V) of the reaction mixture formed in step 1) with hydrogen in the presence of a transition metal catalyst in a solvent or a solvent mixture with or without the presence of an acid to form said Compound (I), and
- 3) optionally adding an acid to precipitate said formed Compound (I) as a salt, wherein said Compound (I), Compound (III), Compound (IV) and Compound (V) are:
A process for the preparation of Compound (V)
- comprising the steps of:
- a) Mixing Compound (III) and Compound (IV) in a solvent or solvent mixture, with or without azeotropical separation of water;
- and
- b) Isolating the precipitated Compound (V);
- wherein said Compound (III) and Compound (IV) are:
2 more elements
Dependencies are inferred from the claim text.