Cc-1065 analog synthesis

C - Chemistry – Metallurgy – 07 – D

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C07D 209/56 (2006.01) C07C 223/06 (2006.01) C07D 209/60 (2006.01)

Patent

CA 2456453

Improved synthesis of seco(-)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2- dihydro-3H-benz(e)indole) (I) and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.

La présente invention concerne une synthèse améliorée de séco(-) CBI (5-hydroxy-3-amino-1[S]-(chlorométhyl)-1,2-dihydro-3H-benz(e)indole): et des synthèses améliorées issues de ces composés d'une grande variété d'analogues CC-1065 qui comprend une fraction d'alkylation cyclopropabenzidole (CBI) et qui sont collectivement DC1 et ses dérivés, ces analogues étant destinés à la synthèse d'agents thérapeutiques à ciblage cellulaire.

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