Process for preparing optically active trans-3-...

C - Chemistry – Metallurgy – 12 – P

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C12P 41/00 (2006.01) C07D 281/02 (2006.01) C07D 281/10 (2006.01) C07D 303/48 (2006.01) C12P 17/02 (2006.01)

Patent

CA 2199880

The present invention is directed to a process for preparing optically active trans-3-phenylglycidamide compound, which comprises subjecting a racemic trans-3-phenylglycidamide compound of the formula (I) Image (I) wherein ring A is substituted or unsubstituted benzene, and R1 is H or lower alkyl, to optical resolution using a microorganism having the ability to preferentially hydrolyze one of (2S,3R) isomer or (2R,3S) isomer thereof, and process for preparing an optically active 1,5-benzothiazepine derivative from the thus-obtained optically active trans-3-phenylglycidamide compound. The 1,5-benzothiazepine derivatives of the present invention are useful as medicaments.

La présente invention porte sur un procédé pour préparer un composé de trans-3-phénylglycidamide optiquement actif, qui consiste à soumettre un composé racémique de trans-3-phénylglycidamide de formule (I) Image (I) dans lequel le noyau A est un benzène substitué ou non substitué, et R1 est un atome de H ou un alkyle inférieur, à une résolution optique à l'aide d'un microorganisme ayant la faculté d'hydrolyser préférentiellement un isomère (2S,3R) ou un isomère (2R,3S) de ce dernier, et sur un procédé pour préparer un dérivé optiquement actif de la 1,5-benzothiazépine à partir du composé trans-3-phénylglycidamide optiquement actif ainsi obtenu. Les dérivés de la 1,5-benzothiazépine de la présente invention sont utiles comme médicaments.

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