Processes for the preparation of...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 301/26 (2006.01) C07D 301/32 (2006.01) C07D 303/36 (2006.01)

Patent

CA 2325919

The present invention provides a production method of high quality threo-1,2-epoxy-3-amino-4-phenylbutane derivatives (1) on a commercial scale in a simple, easy and efficient manner and with very high productivity, which comprises treating a threo-1-halo-2-hydroxy-3- amino-4-phenylbutane derivative (2) with a base in a polar organic solvent or a solvent composed of a polar organic solvent and water, and adding the resulting reaction mixture to water to thereby cause the resulting threo-1,2-epoxy-3-amino-4- phenylbutane derivative (1) to crystallize out.

L'invention concerne un procédé de préparation de dérivés de thréo-1,2-époxy-3-amino-4-phénylbutane (1) de haute qualité, simple, efficace et avec une productivité extrêmement élevée d'un point de vue commercial. Ce procédé consiste à traiter un dérivé de thréo-1-halo-2-hydroxy-3-amino-4-phénylbutane (2) avec une base dans un solvant organique polaire ou un mélange solvant contenant un solvant organique polaire et de l'eau, puis à ajouter le fluide issu de cette réaction à de l'eau en vue de cristalliser un dérivé de thréo-1,2-époxy-3-amino-4-phénylbutane.

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