Process for the preparation of optically pure isomers of...

C - Chemistry – Metallurgy – 07 – C

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C07C 231/18 (2006.01) C07C 205/37 (2006.01) C07C 205/45 (2006.01) C07C 213/02 (2006.01) C07C 217/86 (2006.01) C07C 233/25 (2006.01) C07C 233/43 (2006.01) A61K 9/00 (2006.01)

Patent

CA 2271004

A method is disclosed for the preparation of optically pure isomes of formeterol, especially the (R,R)- and (S,S)-isomer, by the reaction of an optically pure 4-benzyloxy-3- formamidostyrene oxide with an optically pure 4-methoxy-.alpha.-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as is the novel L-tartrate salt of R,R-formoterol.

L'invention concerne une procédé pour préparer des isomères de formotérol optiquement purs, en partiucler les isomères (R,R) et (S,S), par réaction d'un oxyde 4-benzyloxy-3-formamidostyrène optiquement pur avec une 4-méthoxy- alpha -méthyl-N-(phénylméthyl)benzèneéthanamine optiquement pure, puis par débenzylation. L'invention concerne également des intermédiaires utiles audit procédé, comme peut l'être le nouveau sel de L-tartrate de R,R-formotérol.

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