SPERGUALIN-RELATED COMPOUND AND PREPARATION THEREOF

摘要

NEW MATERIAL:A compound of formula I (R1 is H, hydroxyl or 1-10C aliphatic acyloxy; R2 is a residue, obtained by removing one H and hydroxyl from the carboxyl group of an alpha- or omega-amino group in an alpha- or omega-amino acid except alpha-hydroxyglycine residue, and linked to the adjacent carbonyl group and amino group; m is an integer 4-6). EXAMPLE:10-[N-(7-Guanidinoheptanoyl)glycyl]-1,5,10-triazadecane. USE:A medicine, expected as an antitumor agent, etc., and having improved biological activity and stability. PROCESS:The protecting groups are removed from a novel protected spergualin- related compound of formula II (R2' is the same as R<2>; R3 and R4 are protecting groups of the amino groups) by the weel-known method to give the aimed compound of formula I . The compound of formula II is obtained by condensing a 1,5-diprotected-1,5,10-triazadecane of formula III with an N-protected amino acid of the formula R5-OH, removing the protecting group of the amino group in R5, and condensing the resultant compound with an omega-guanidino fatty acid of formula IV.