PROCESS FOR THE PRODUCTION OF ELLIPTICINE GLYCOSIDE FROM AN ELLIPTICINE DERIVATIVE AND ARABINOSE

摘要

PURPOSE:To obtain the titled compound useful as a carcinostatic agent in high yield, by reacting an ellipticine compound with an arabinose derivative in the presence of a trialkylamine as an acid capturing agent in an organic solvent. CONSTITUTION:(A) An ellipticine compound expressed by formula I (R1 is H, OH, 1-3C alkyloxy or 2-8C acyloxy; R2 is H or 1-6C alkyl) is reacted with (B) an arabinose derivative expressed by formula II (R3 is acyl; X is Cl or Br) in the presence of a trialkylamine (preferably triethylamine, tripropylamine, triisopropylamine, diisopropylethylamine or tributylamine) as an acid capturing agent in an organic solvent (preferably acetonitrile, nitromethane or propionitrile) to afford the aimed compound expressed by formula III.