Ro 11-2933, a potential drug in the treatment of cancer and malaria: Synthesis and physicochemical properties; potential metabolites

Article abstract of DOI:10.1016/0223-5234(89)90053-6

Ro 11-2933, 4b, a compound with minor cardiovascular activity has been shown to reverse multidrug resistance in cancer cells as well as chloroquine resistance in Plasmodium falciparum. A useful synthesis of the drug is described. Alkylation of dithiane (2) with chloroalkylamine (3) affords 4b as a crystalline compound in a very good yield. The synthesis of its potential metabolites 7 and 11 has also been carried out.