T-Butyloxy-carbonyl-D-phenylalanyl-L-prolyl-L-arginine aldehyde
hemisulfate, D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate and
process for the preparation thereof
    1.
    发明授权
    T-Butyloxy-carbonyl-D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate, D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate and process for the preparation thereof 失效
    叔丁氧基 - 羰基-D-苯丙氨酰-L-脯氨酰基-L-精氨酸醛半硫酸酯,D-苯丙氨酰-L-脯氨酰-L-精氨酸醛硫酸盐及其制备方法

    公开(公告)号:US4478745A

    公开(公告)日:1984-10-23

    申请号:US484888

    申请日:1983-04-14

    CPC分类号: C07K5/06078 Y02P20/55

    摘要: The invention relates to t-butyloxy-carbonyl-D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate and D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate, which is highly stable in aqueous solution, and to a process for preparing D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate from D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate or N.sup.G -carboxy derivative containing an acid-sensitive protecting group at its amino terminal, wherein the acid sensitive amino terminal protecting group or optionally the N.sup.G -carboxy group is removed with 1 to 12 N sulfuric acid, applied in 1 to 12 equivalent amounts and the resulting free tripeptide aldehyde sulfate isolated. The D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate of the invention possesses valuable anti-coagulant activity.

    摘要翻译: 本发明涉及在水溶液中高度稳定的叔丁氧基 - 羰基-D-苯丙氨酰-L-脯氨酰基-L-精氨酸醛半硫酸酯和D-苯丙氨酰-L-脯氨酰-L-精氨酸醛硫酸酯, 用于由D-苯丙氨酰基-L-脯氨酰基-L-精氨酸醛半硫酸盐或其氨基末端含有酸敏感性保护基的NG-羧基衍生物制备D-苯丙氨酰基-L-脯氨酰基-L-精氨酸醛硫酸酯,其中酸敏感 氨基末端保护基团或任选的NG-羧基用1至12N硫酸除去,以1至12当量的量施用,并且分离所得的游离三肽醛硫酸盐。 本发明的D-苯丙氨酰-L-脯氨酰-L-精氨酸醛硫酸盐具有有价值的抗凝剂活性。

    D-Phenylalanyl-L-prolyl-L-arginine aldehyde sulfate and process for the
preparation thereof
    2.
    发明授权
    D-Phenylalanyl-L-prolyl-L-arginine aldehyde sulfate and process for the preparation thereof 失效
    D-苯丙氨酰-L-脯氨酰-L-精氨酸醛硫酸盐及其制备方法

    公开(公告)号:US4399065A

    公开(公告)日:1983-08-16

    申请号:US337288

    申请日:1982-01-05

    CPC分类号: C07K5/06078 Y02P20/55

    摘要: The invention relates to D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate, highly stable in aqueous solution, and to a process for preparing it from D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate or N.sup.G -carboxy derivative containing an acid-sensitive protecting group at its amino terminal, wherein the acid sensitive amino terminal protecting group or optionally the N.sup.G -carboxy group is removed with 1 to 12 N sulfuric acid, applied in 1 to 12 equivalent amounts and the resulting free tripeptide aldehyde sulfate is isolated. The D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate of the invention possesses valuable anticoagulant activity.

    摘要翻译: 本发明涉及在水溶液中高度稳定的D-苯丙氨酰-L-脯氨酰基-L-精氨酸醛硫酸酯,以及由D-苯丙氨酰-L-脯氨酰基-L-精氨酸醛半硫酸酯或NG-羧基衍生物制备的方法 在其氨基末端含有酸敏感性保护基,其中用1至12N硫酸除去酸敏感氨基末端保护基团或任选的NG-羧基基团,以1至12当量施用,得到的游离三肽醛 分离出硫酸盐。 本发明的D-苯丙氨酰-L-脯氨酰-L-精氨酸醛硫酸盐具有有价值的抗凝血活性。