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US 2013/0158256 A1Published application
Process for the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
AssigneeLes Laboratoires Servier
InventorsJean-Luc RENAUD, Nicolas Pannetier, Jean-Pierre Lecouve, Lucile Vaysse-Ludot, Solenne Moulin
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Abstract
Process for the synthesis of ivabradine of formula (I): addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.
Claims15
A process for the synthesis of ivabradine of formula (I):
- wherein a compound of formula (V):
- is subjected to a reductive amination reaction with an amine of formula (VI):
- in the presence of an iron-based catalyst,
- optionally in the presence of trimethylamine N-oxide,
- under dihydrogen pressure of from 1 to 20 bars,
- in an organic solvent or mixture of organic solvents,
- at a temperature from 25 to 100° C.
4 more elements
Dependencies are inferred from the claim text.