| 摘要 |
<p>PURPOSE:To obtain the titled compound useful as an antitumor agent, by a method suitable for mass-synthesis, in a relatively short reaction period, by guanidinating a triazadecane derivatve, and removing the protecting group. CONSTITUTION:The novel 10-[N-(omega-(4-aminophenyl)acyl)aminoacyl]-1,5-diprotected 1,5,10-triazadecane of formula I (R'1 is residue obtained by removing one H atom from the amino group and removing hydroxyl group from the carboxyl group of glycine or serine, or R'1 forms an acid amide bond with adjacent carbonyl and amino group; R2 is amino-protecting group; m is 3-5) is made to react with a guanidination reagent in an organic solvent at >=0 deg.C, and the protecting group is removed from the reaction product to obtain the objective compound of formula II. The amount of the guanidination reagent is >=0.5mol, preferably 1,2-3mol per 1mol of the compound of formula I.</p> |
