One-pot microwave-assisted synthesis and antimalarial activity of ferrocenyl benzodiazepines

Abstract

An efficient synthesis of 1,4-benzodiazepin-2-ones is described by condensation between 2-aminobenzophenone and Boc-protected amino acids via microwave-assisted irradiation. This produces higher yields in shorter reaction times than with traditional methods. The antiplasmodial activity of the corresponding ferrocenyl benzodiazepines was evaluated in vitro against Plasmodium falciparum F32 (chloroquine-sensitive) and FCB1 and K1 (chloroquine-resistant) strains and gabonese clinical isolates.