Solid-phase synthesis method of Ziconotide



The invention discloses a solid-phase synthesis method of Ziconotide. The method comprises the following steps of: performing condensation reaction by taking Fmoc-amino resin as a solid-phase carrier and connecting 25 side chain protected amino acids to obtain linear fully protected resin, wherein three groups of Cys which form disulfide bonds are connected with Trt, Acm or tBu protecting groups respectively; linearly cutting the resin and removing the side chain protected groups of other amino acids except for Cys(Acm) and Cys(tBu); oxidizing linear peptide to form the first pair of disulfide bonds to obtain single disulfide cyclopeptide; removing the Acm protected group of the Cys(Acm) from the single disulfide cyclopeptide and cyclizing to form the second pair of disulfide bonds to obtain double disulfide cyclopeptide; removing the tBu protected group of the Cys(tBu) from the double disulfide cyclopeptide and cyclizing to form the third pair of disulfide bonds to obtain triple disulfide cyclopeptide; and purifying and freeze-drying the triple disulfide cyclopeptide to obtain the Ziconotide.




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Patent Citations (2)

    Publication numberPublication dateAssigneeTitle
    CN-101412752-AApril 22, 2009杭州诺泰制药技术有限公司齐考诺肽的固相合成方法
    CN-102268082-ADecember 07, 2011江苏江神药物化学有限公司一种齐考诺肽的固相合成方法

NO-Patent Citations (1)

    曹本文: "选择性氧化形成三对二硫键合成齐考诺肽", 《合成化学》, vol. 19, no. 1, 31 January 2011 (2011-01-31), pages 145 - 147

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    CN-104974229-AOctober 14, 2015泰州施美康多肽药物技术有限公司Linaclotide solid-phase synthesis method