Facile and improved synthesis of 4β-aminopodophyllotoxin congeners

Article abstract of DOI:10.1016/S0960-894X(98)00570-8

An efficient synthesis of 4β-aminopodophyllotoxin from 4β- bromopodophyllotoxin using ammonia, and also a facile synthesis of 4β- amino-4'-O-demethylpodophyllotoxin from 4β-azidopodophyllotoxin by simultaneous azido reduction and selective demethylation at 4'-position employing chlorotrimethylsilane and sodium iodide, has been described. These are potential precursors for the various 4β-amino analogs of podophyllotoxin possessing DNA topoisomerase II inhibition activity.