DERIVES DE 11-HYDROXY-5H-PYRROLO[2,1-C][1,4] BENZODIAZEPINE-5-ONE EN TANT QU'INTERMEDIAIRES CLES POUR LA PREPARATION DE PYRROLOBENZODIAZEPINES SUBSTITUEES C2
The present inventors have developed a key intermediate for the production ofC2 substituted PBDs, which has a leaving group at the C2 position, a carbamateprotecting group at the N10 position and a protected hydroxy group at the C11position. In a first aspect, the present invention comprises a compound with athe formula (I), wherein : R10 is a carbamate-based nitrogen protecting group；R11 is an oxygen protecting group； and R2 is a labile leaving group. In afurther aspect, the present invention comprises a method of synthesising acompound of formula (III), or a solvate thereof, from a compound of formula(I) as defined in the first aspect, R16 is either O-R11, wherein R11 is asdefined in the first aspect, or OH, or R10 and R16 together form a double bondbetween N10 and C11； and R15 is R. The other substituents are defined in theclaims. Further aspects of the present invention relate to compounds offormula (III) (including solvates thereof when R10 and R16 form a double bondbetween N10 and C11, and pharmaceutical salts thereof), pharmaceuticalcompositions comprising these, and their use in the manufacture of amedicament for the treatment of a proliferative disease.
