Process for producing triglycyl-lysine vasopressin and intermediates
therefor
    2.
    发明授权
    Process for producing triglycyl-lysine vasopressin and intermediates therefor 失效
    制备三甘氨酰赖氨酸加压素及其中间体的方法

    公开(公告)号:US4093610A

    公开(公告)日:1978-06-06

    申请号:US763772

    申请日:1977-01-31

    CPC分类号: C07K7/16 A61K38/00 Y10S930/15

    摘要: A new process for preparing the cyclic dodecapeptide triglycyl-lysine vasopressin of the formula ##STR1## which comprises the preparation of a first hexapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--NHNH.sub.2 and a second hexapeptide of formula H--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 by a series of condensations involving the reaction of an appropriately protected peptide unit having an activated carboxyl with an appropriately protected peptide having a free amino group. Subsequently, the first and second hexapeptides are condensed according to the azide coupling method to obtain the linear protected dodecapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 ; thereafter the linear protected dodecapeptide is transformed into the desired cyclic dodecapeptide, triglycyllysine vasopressin, by oxidizing and deprotecting processes.

    摘要翻译: 制备式“IMAGE”的环十二肽三缩水甘油基赖氨酸加压素的新方法,其包括制备式Boc-Gly-Gly-Gly-Cys(Trt)-Tyr-Phe-NHNH 2的第一六肽和第二个六肽 通过一系列缩合产生式H-Gln(Mbh)-Asn(Mbh)-Cys(Trt)-Pro-Lys(Boc)-Gly-NH 2)的反应,该缩合涉及适当保护的具有活性羧基的肽单元与适当的 具有游离氨基的保护肽。 随后,根据叠氮偶合法将第一和第二六肽缩合,得到式Boc-Gly-Gly-Gly-Cys(Trt)-Tyr-Phe-Gln(Mbh)-Asn(Mbh) - Cys(Trt)-Pro-Lys(Bo c)-Gly-NH 2; 此后,通过氧化和脱保护过程将线性保护的十二肽转化成所需的环十二肽,甘氨酰赖氨酸加压素。