DECAPEPTIDE
    11.
    发明专利

    公开(公告)号:JPS58152850A

    公开(公告)日:1983-09-10

    申请号:JP3403182

    申请日:1982-03-05

    申请人: EISAI CO LTD

    IPC分类号: C07K7/06

    摘要: NEW MATERIAL:The decapeptide of formulaI(X is H or benzyloxycarbonyl) and its salt. USE:Synthetic intermediate of secretin. The fragment of formulaI is condensed with the novel fragment of formula II, and the resultant novel fragment of formula III is condensed with the novel fragment of formula IV to obtain protected secretin, from which all protecting groups are removed in one step to obtain secretin easily. PROCESS:The protected amino acid of formula Z-Arg(Tos)-OH is dissolved in DMF, added with N-methylmorpholine, and reacted with isobutyl chlorophosphate under cooling to obtain an active-type anhydride mixture. Separately, the peptide of formula V is dissolved in DMF and mixed with N-methylmorpholine. The mixture is mixed with the above anhydride mixture and condensed to obtain the decapeptide of formulaI. The peptide of formula V can be prepared by reducing the Z-compound in HCl and trifluoroethanol in the presence of a catalyst.

    HEPTAPEPTIDE
    12.
    发明专利

    公开(公告)号:JPS58152848A

    公开(公告)日:1983-09-10

    申请号:JP3402982

    申请日:1982-03-05

    申请人: EISAI CO LTD

    IPC分类号: C07K7/06

    摘要: NEW MATERIAL:The heptapeptide of formulaI(X is H or benzyloxycarbonyl). USE:Synthetic intermediate of secretin. The fragment of formulaI is condensed with the novel fragment of formula II, and the resultant novel fragment of formula III is condensed with the novel fragment of formula IV to obtain a protected secretin, from which all protecting groups are removed in one step to obtain secretin easily. PROCESS:The Z-removed compound of the peptide of formula V is condensed with the peptide of formula VI to obtain the heptapeptide of formulaI. The reaction is carried out by dissolving the peptide of formula VI and N-hydroxysuccinimide in DMF, adding DCC as a condensation agent to the solution, and condensing the product with the Z-removed compound of the peptide of formula V obtained by removing the protecting group by reduction. The peptide of formula V can be prepared by reacting the protected arginine of formula Z- Arg(Tos)-OH with the peptide of formula VII.

    PREPARATION OF SECRETIN
    13.
    发明专利

    公开(公告)号:JPS58144355A

    公开(公告)日:1983-08-27

    申请号:JP2608882

    申请日:1982-02-22

    申请人: EISAI CO LTD

    摘要: PURPOSE:To obtain the titled compound useful as an agent for testing pancreatic function, etc., at low temperature, in a short time, in high activity and purity, with simple purification process, without side reactions, by removing the protecting group of a novel heptacosapeptide having a specific structural formula. CONSTITUTION:Secretin is prepared by removing the protecting group from a heptacosapeptide having a novel structural formula (Boc, His, etc. are abbreviations of tert-butyloxycarbonyl, histidine, etc. which are widely used in the field of peptide chemistry). The removel of the protecting group is preferably carried out in a short time, in one step by treating the compound with a strong acid (e.g. trifluoromethanesulfonic acid, hydrogen fluoride, etc.). The characteristic feature of the compound is the protection of the amino group of the N-terminal and the side chain functional groups of all constituent amino acids of secretin.

    Heptacosapeptide
    17.
    发明专利
    Heptacosapeptide 失效
    HEPTACOSAPEPTIDE

    公开(公告)号:JPS5750947A

    公开(公告)日:1982-03-25

    申请号:JP12526280

    申请日:1980-09-11

    申请人: Eisai Co Ltd

    摘要: NEW MATERIAL:A heptacosapeptide of formula I (Boc is tert-butyloxycarbonyl; Bu
    t is tert-butyl; OBu
    t is tert-butyl ester; Tos is tosyl).
    USE: A synthetic intermediate for secretin, characterized by the combination of a specific protecting group, and capable of releasing the whole protecting groups readily easily at a low temperature in a short time by using HF and giving secretin of high activity and high purity by a simple purifying method. The secretin is a kind of digestive tract hormone and useful as a pancreatic function testing agent, remedy for the duodenal ulcer, etc.
    PROCESS: A decapeptide of formula II is condensed with a heptadecapeptide of formula III to give the heptacosapeptide of formula I.
    COPYRIGHT: (C)1982,JPO&Japio

    摘要翻译: 新物质:式I的七肽(Boc是叔丁氧羰基; Bu t是叔丁基; OBu是叔丁酯; Tos是甲苯磺酰基)。 用途:用于促胰液素的合成中间体,其特征在于特异性保护基团的组合,并能够通过使用HF在短时间内容易地在低温下释放整个保护基团,并通过使用HF并且通过使用HF来提供高活性和高纯度的促胰液素 简单净化方法。 胰泌素是一种消化道激素,可用作胰腺功能测试剂,十二指肠溃疡等的治疗方法。方法:将式II的十肽与式III的十七肽缩合,得到式I的十七肽。