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    Process for Synthesis of Cyclic Octapeptide
    7.
    发明申请
    Process for Synthesis of Cyclic Octapeptide 有权
    环十八肽合成方法

    公开(公告)号：US20120035117A1

    公开(公告)日：2012-02-09

    申请号：US13123623

    申请日：2009-05-04

    申请人： Divya Lal Saksena ,  Digamber Shripati Pawar ,  Nikhil Umesh Mohe ,  Nilesh Dagdu Patil ,  Chandrakesan Muralidharan ,  Lester Lobo ,  Radhakrishnan Venkatasubramanian Tarur

    发明人： Divya Lal Saksena ,  Digamber Shripati Pawar ,  Nikhil Umesh Mohe ,  Nilesh Dagdu Patil ,  Chandrakesan Muralidharan ,  Lester Lobo ,  Radhakrishnan Venkatasubramanian Tarur

    IPC分类号： A61K38/08 ,  C07K7/06 ,  C07K1/10

    CPC分类号： C07K14/6555 ,  A61K38/00

    摘要： This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide. Alternatively threoninol is coupled to the heptapeptide of formula (3) to yield protected octapeptide of formula (4) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-Thr-OL which is subsequently deprotected to yield linear octapeptide of formula (5) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL and cyclized with hydrogen peroxide to yield cyclic octreotide with a yield of >95%.

    摘要翻译： 本发明涉及制备奥曲肽及其衍生物的方法。 将起始物质Cys（Trt）-2-氯三苯甲基树脂与各种氨基酸偶联得到式（2）的保护的七肽：Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc ）-Thr（OBut）-Cys（Trt）-2-氯三苯甲基树脂。 使用TFA5TIS和水从支持物上切割式（2）的线性保护肽，得到式（3）的线性保护肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc） - Thr（OBut）-Cys（Trt）-OH将式（3）的线性保护的七肽脱保护得到式（6）的七肽：D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; 其使用过氧化氢和式（7）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH的环肽环化; 苏氨酚在C末端偶联以产生奥曲肽。 或者，苏糖醇与式（3）的七肽偶联以得到式（4）的保护的八肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc）-Thr（OBut）-Cys Trt）-Thr-OL，随后脱保护得到式（5）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL的直链八肽，并用过氧化氢环化，得到环状奥曲肽， 产量> 95％。

    Process for synthesis of cyclic octapeptide
    8.
    发明授权
    Process for synthesis of cyclic octapeptide 有权
    合成八肽的方法

    公开(公告)号：US08377891B2

    公开(公告)日：2013-02-19

    申请号：US13123623

    申请日：2009-05-04

    申请人： Divya Lal Saksena ,  Digamber Shripati Pawar ,  Nikhil Umesh Mohe ,  Nilesh Dagdu Patil ,  Chandrakesan Muralidharan ,  Lester Lobo ,  Radhakrishnan Venkatasubramanian Tarur

    发明人： Divya Lal Saksena ,  Digamber Shripati Pawar ,  Nikhil Umesh Mohe ,  Nilesh Dagdu Patil ,  Chandrakesan Muralidharan ,  Lester Lobo ,  Radhakrishnan Venkatasubramanian Tarur

    IPC分类号： A61K38/08

    CPC分类号： C07K14/6555 ,  A61K38/00

    摘要： This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide. Alternatively threoninol is coupled to the heptapeptide of formula (3) to yield protected octapeptide of formula (4) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-Thr-OL which is subsequently deprotected to yield linear octapeptide of formula (5) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL and cyclized with hydrogen peroxide to yield cyclic octreotide with a yield of >95%.

    摘要翻译： 本发明涉及制备奥曲肽及其衍生物的方法。 将起始物质Cys（Trt）-2-氯三苯甲基树脂与各种氨基酸偶联得到式（2）的保护的七肽：Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc ）-Thr（OBut）-Cys（Trt）-2-氯三苯甲基树脂。 使用TFA5TIS和水从支持物上切割式（2）的线性保护肽，得到式（3）的线性保护肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc） - Thr（OBut）-Cys（Trt）-OH将式（3）的线性保护的七肽脱保护得到式（6）的七肽：D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; 其使用过氧化氢和式（7）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH的环肽环化; 苏氨酚在C末端偶联以产生奥曲肽。 或者，苏糖醇与式（3）的七肽偶联以得到式（4）的保护的八肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc）-Thr（OBut）-Cys Trt）-Thr-OL，随后脱保护得到式（5）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL的直链八肽，并用过氧化氢环化，得到环状奥曲肽， 产量> 95％。

    Solid phase Fmoc chemistry process to prepare peptides
    9.
    发明授权
    Solid phase Fmoc chemistry process to prepare peptides 失效
    固相Fmoc化学过程制备肽

    公开(公告)号：US07897724B2

    公开(公告)日：2011-03-01

    申请号：US11729047

    申请日：2007-03-27

    申请人： Divya Lal Saksena ,  Shrikant Mishra ,  Chandrakesan Muralidharan ,  Nilesh Patil ,  Nikhil Umesh Mohe ,  Mandar Ravindra Maduskar

    发明人： Divya Lal Saksena ,  Shrikant Mishra ,  Chandrakesan Muralidharan ,  Nilesh Patil ,  Nikhil Umesh Mohe ,  Mandar Ravindra Maduskar

    IPC分类号： C07K1/06

    CPC分类号： C07K14/75 ,  C07K14/78 ,  Y02P20/582

    摘要： The present invention relates to an improved process for the preparation of N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-L-lysylglycyl-L-α-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic(1→6)-disulfide of formula (1), which involves assembling a peptide chain comprising of six amino acids and a thioalkyl carboxylic acid in a required sequence on a solid support to obtain a peptide bound resin of formula (2), capping the free amino groups after each coupling, cleaving Dde group in the peptide of formula (2) from the solid support to obtain peptide-solid support of formula (3), guanylating the peptide of formula (3) at ε-lysine-NH2 in an organic solvent to obtain peptide-solid support of formula (4), cleaving and deprotecting all groups in the peptide of formula (4) from the solid support to obtain peptide-amide formula (5), oxidizing the SH-peptide of formula (5) with an appropriate oxidizing agent to obtain the crude peptide-amide of formula (1) and purifying the crude peptide-amide of formula (1) by chromatographic technique. The solid support is either resin or a cellulose support like cotton, gauze, fabric, paper and perloza beads. The described process is simple, easy, environment friendly, takes lesser time and more cost effective.

    摘要翻译： 本发明涉及一种制备N6-（氨基亚氨基甲基）-N2-（3-巯基-1-氧代丙基）-L-赖氨酰甘氨酰-L-α-天冬氨酰-L-色氨酰-L-脯氨酰基-L- 半胱氨酰胺，式（1）的环状（1→6） - 二硫化物，其包括在固体支持物上以所需的顺序将包含六个氨基酸的肽链和硫代烷基羧酸组装以获得式（2）的肽结合树脂 ），在每次偶联后封端游离氨基，从固体支持物切割式（2）的肽中的Dde基团以获得式（3）的肽 - 固体支持物，在式（3）的肽上进行脒化， 赖氨酸-NH 2在有机溶剂中得到式（4）的肽固体支持物，从固体支持物中切割和脱保护基团中所有基团的肽，得到肽 - 酰胺式（5），氧化SH- 式（5）的肽与适当的氧化剂反应，得到式（1）的粗肽 - 酰胺并纯化粗蛋白 e通过色谱技术制备式（1）的肽 - 酰胺。 固体支持物是树脂或纤维素载体，如棉，纱布，织物，纸和perloza珠。 描述的过程简单，容易，环保，花费更少的时间和更具成本效益。