| 摘要 |
PURPOSE:To improve the stability in the blood and avoid the nonspecific adhesion to internal organs by modifying the epsilon-amino group of polylysine with a group containing ethylene glycol. CONSTITUTION:Polylysine is reacted with an acid azide derived from a compound of formula I (wherein R<1> is glycosyl) to introduce a sugar chain. The reaction product is reacted with a compound of formula II (wherein R<3> is H or a drug residue) by using hydroxysuccinimide ester and a condensing agent, such as DCC, and then reacted with oxysuccinimide ester of formula III (wherein R<2> is a group of formula IV or V; and n is 1 or 2) to give a sugar-modified polylysine derivative of formula VI (wherein X is a group of formula VII; k is 2 to 8; m is 0 to 2; and p, q and r are the numbers of structural units A, B and C and are respectively 1 to 200, 10 to 300, and 1 to 20), consisting of the structural units A, B and C and having a molecular weight of 5,000 to 150,000. |
