| 摘要 |
PURPOSE:To provide a new derivative useful as a vascularization inhibitor. CONSTITUTION:The objective derivative of formula I (R<1> is H, lower alkoxycarbonyl, etc.; R<2> is OH, amino, etc.; l and m are each 0-8; (l+m)=3-8; amino acid residues are each D-modification, L-modification, or a mixture thereof) or a medically permissible salt thereof, e.g. a compound of formula II (Arg is arginine residue; Boc is t-butoxycarbonyl; phGly is alpha-phenylglycine residue; Asp is aspartic acid residue; Gly is glycine residue). The compound of the formula I can be obtained, for example, by condensation reaction between a compound of formula III (Asp is aspartic acid residue; OBzl is benzyloxy; OBu<t> is t-butoxy) and a compound of formula IV followed by deprotection to produce a compound of formula V, which is then further condensed with a compound of formula VI (OBzI is benzyloxy; TsOH is p-toluenesulfonic acid) to deprotect the N- terminal and C-terminal and reprotect the N-terminal. |
