Process for preparation of cyclosporin "a" analogues having...

Details Process for preparation of cyclosporin "a" analogues having... Process for preparation of cyclosporin "a" analogues having...

C - Chemistry, Metallurgy

07

K

C07K 7/64 (2006.01) C07F 5/02 (2006.01)

Patent

CA 2521116

The invention is concerned with a new process for the preparation of a cyclosporin A analog of formula I comprising, a) allylating a protected cyclosporin A aldehyde with a allylmetal reagent and, b) converting the compound obtained in step a) to the cyclosporin A analog of formula I. In particular, the allyl reagent is a trimethylsilyl-allyl borate ester or a trimethylsilyl-allyl organometallic compound containing aluminium or titanium.

La présente invention concerne un nouveau procédé pour préparer un analogue de la cyclosporine A de formule I, comprenant les étapes suivantes: a) allylation d'un aldéhyde de cyclosporine A protégé avec un réactif d'allylation; et b) conversion du composé obtenu dans l'étape a) en l'analogue de cyclosporine A de formule I.

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