Process for producing optically active...

C - Chemistry – Metallurgy – 07 – D

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C07D 301/02 (2006.01) C07B 53/00 (2006.01) C07D 303/36 (2006.01)

Patent

CA 2319088

Highly pure optically active threo-3-amino-1,2-epoxy compounds appropriate for materials for manufacturing drugs and a process for producing the same on an industrial scale. An optically active threo-3-amino-1,2-diol derivative is subjected in an organic solvent in the presence of a base to alkylsulfonylation or arylsulfonation to thereby give the corresponding optically active threo-3-amino-2-hydroxy-1-sulfonyloxy compound. Next, the resultant product is subjected to epoxidation in the presence of a base to give the corresponding optically active threo-3-amino-1,2-epoxy compound. The thus obtained epoxy compound is purified by using an organic solvent and water, thus giving a highly pure epoxy compound.

Composés de threo-3-amino-1,2-epoxy optiquement actifs, extrêmement purs et appropriés pour des matériaux servant à préparer des médicaments et procédé servant à produire ces composés à l'échelle industrielle. On soumet un dérivé de threo-3-amino-1,2-diol à une alkylsufonylation ou arylsulfonylation dans un solvant organique en présence d'une base, de manière à obtenir le composé correspondant optiquement actif de threo-3-amino-2-hydroxy-1-sulfonyloxy. On soumet ensuite le produit obtenu à une époxydation en présence d'une base, de manière à produire le composé correspondant optiquement actif de threo-3-amino-1,2-epoxy. On purifie le composé époxydique obtenu de cette façon au moyen d'un solvant organique et d'eau, ce qui permet d'obtenir un composé époxydique extrêmement pur.

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