Production of 6-oacylelsamycin a derivative

PURPOSE: To obtain the subject compd. for a low-toxicity antitumor agent, etc., by treating a 2"-Nt-butoxycarbonylelsamycin A with an alkyl halide in the presence of KI in dimethyl sulfoxide, etc., subjecting the product to a trifluoroacetic acid treatment. CONSTITUTION: The 2"-Nt-butoxycarbonylelsamycin A prepd. by stirring overnight a mixture composed of an elsamycin A, di-tbutyldicarbonate and triethylamine at room temp. in a dioxane, subjecting the reaction mixture to reduced pressure concentration and recrystallizing the residue from dimethyl chlorometa/ether is treated with an alkyl halide (e.g: methyl iodide, etc.) in the presence of potassium iodide and/or potassium carbonate to obtain the corresponding 6-O-alkyl deriv. and is in succession treated with trifluoroacetic acid, by which the objective 6-O-acylelsamycin A deriv. expressed by the formula [R is a 1 to 10C alkyl, a (substd.) aminoalkyl] and exhibiting the excellent antitumor activity is obtd. COPYRIGHT: (C)1993,JPO