Method of preparing poly(adp-ribose) polymerases inhibitors

Details Method of preparing poly(adp-ribose) polymerases inhibitors Method of preparing poly(adp-ribose) polymerases inhibitors

C - Chemistry, Metallurgy

07

D

C07D 487/06 (2006.01) C07D 209/00 (2006.01) C07D 223/00 (2006.01)

Patent

CA 2580833

The invention relates to a new and convergent route to small molecule inhibitors of poly(ADP-ribose) polymerase, such as 8-fluoro-2{4- [(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino [5,4,3-cd]indol-6- one, via a key Sonogashira coupling reaction and a Cul-promoted indole formation.

Nouvelle voie convergente vers des inhibiteurs à petites molécules de poly(ADP-ribose) polymérase, tels que la -fluoro-2{4-[(méthylamino)méthyl]phényl}-1,3,4,5-tétrahydro-6H-azépino [5,4,3-cd]indol-6-one, via une réaction clé de couplage de Sonogashira et une formation d'indole favorisée par Cul.

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