[EN] PHENYL-SULFAMATES AS AROMATASE INHIBITORS<br/>[FR] PHENYL-SULFAMATES EN TANT QU'INHIBITEURS DE L'AROMATASE
申请人:STERIX LTD
公开号:WO2005118560A1
公开(公告)日:2005-12-15
There is provided a compound of Formula (I) wherein X, Y and Z are each independently of each other an optional linker group; R, is a ring system; R2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (CN), nitro (-NO2) and halogens; R3 and R4 are independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.
There is provided a compound of Formula I
wherein X, Y and Z are each independently of each other an optional linker group; R
1
is a ring system; R
2
is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO
2
) and halogens; R
3
and R
4
are independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.
There is provided a compound of Formula I
wherein X, Y and Z are each independently of each other an optional linker group; R
1
is a ring system; R
2
is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO
2
) and halogens; R
3
and R
4
are independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.
Rh-catalyzed cyano transfer reaction between alkynyl-malononitrile derivatives and aryl/alkenyl boronic acids. This reaction exhibits high chemo- and regioselectivity and a broad substrate scope. The tetrasubstituted alkenyl dinitriles (34 examples, average 58% yield) are obtained through substrate tuning and ligand control.