申请人:DAICEL CHEMICAL INDUSTRIES, LTD.
公开号:EP0452514A1
公开(公告)日:1991-10-23
A peptide represented by general formula (I) is cyclized to give a cyclic peptide, preferably a synthetic calcitonin derivative (elcatonin). In the formula, A and B form a peptide represented by the formula Ser-Asn-Leu-Ser-Thr and X is a hydroxyl group, a protective group for a carboxyl group, an amino acid residue or a peptide residue, provided that an amino acid or a peptide is condensed with the side chain carboxyl group of a-L-aminosuberic acid. The cyclic peptide is prepared by subjecting the peptide represented by general formula (I) to (1) a cyclization reaction through a chemical condensation, (2) a cyclization reaction in the presence of an alkali metal salt and (3) a reaction comprising a combination of a liquid-phase synthesis with a solid-phase synthesis.
将通式(I)所代表的肽环化,得到环肽,最好是合成降钙素衍生物(elcatonin)。式中,A 和 B 形成由式 Ser-Asn-Leu-Ser-Thr 表示的肽,X 是羟基、羧基的保护基、氨基酸残基或肽残基,条件是氨基酸或肽与 a-L-aminosuberic acid 的侧链羧基缩合。环肽的制备方法是将通式(I)代表的肽进行(1)化学缩合的环化反应,(2)碱金属盐存在下的环化反应,(3)液相合成与固相合成相结合的反应。