Method for producing l-phenylephrine hydrochloride

Details Method for producing l-phenylephrine hydrochloride Method for producing l-phenylephrine hydrochloride

C - Chemistry, Metallurgy

07

C

C07C 215/60 (2006.01) C07C 213/08 (2006.01)

Patent

CA 2355938

The present invention relates to an improved process for preparing L- phenylephrine hydrochloride 3 on an industrial scale by asymmetric hydrogenation as the key step and a special sequence of subsequent steps, using [Rh(COD)Cl]2 as catalyst and a chiral, two-pronged phosphine ligand such as (2R, 4R)-4-(dicyclohexylphosphino)-2- (diphenylphosphino-methyl)-N-methyl-aminocarbonyl-pyrrolidine as the catalyst system.

L'invention concerne une amélioration apportée à un procédé de préparation d'hydrochlorure de L-phényléphrine 3 à l'échelle industrielle, ledit procédé faisant appel à une hydrogénation asymétrique comme étape principale et à une série d'étapes suivantes. Selon l'invention, on utilise, comme catalyseur, du [Rh(COD)Cl]2 et, comme système catalyseur, un ligand de phosphine chiral bidentate tel que la (2R, 4R)-4-(dicyclohexylphosphino)-2-(diphénylphosphino-méthyl)-N-méthyl-aminocarbonyl-pyrrolidine.

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