Convenient synthesis of pyrrolo[3,4-g]indazole
- Autori: Spano', V.; Montalbano, A.; Carbone, A.; Parrino, B.; Diana, P.; Cirrincione, G.; Barraja, P.
- Anno di pubblicazione: 2013
- Tipologia: Articolo in rivista (Articolo in rivista)
- Parole Chiave: Tetrahydropyrrolo[3,4-g]indazole, Hydroxymethyleneketones, Antiproliferative activity, Regioselectivity
- OA Link: http://hdl.handle.net/10447/83483
The synthesis of a novel class of tetrahydropyrrolo[3,4-g]indazoles is reported, by annelation of the pyrazole ring on the isoindole moiety by means of 5-hydroxymethylene tetrahydroisoindole-4-ones key intermediates, with good regioselectivity. Dihydroderivatives were also obtained by oxidation with DDQ of the corresponding tetrahydropyrrolo[3,4-g]indazoles. The growth inhibitory effect was evaluated at the National Cancer Institute of Bethesda and some derivatives showed modest activity.