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1. 发明授权

US08829157B2 Process for the synthesis of cyclic heptapeptide 有权
标题翻译：用于合成环七肽的方法
公开(公告)号：US08829157B2
公开(公告)日：2014-09-09
申请号：US13007736
申请日：2011-01-17
申请人： Divya Lal Saksena , Chandrakesan Muralidharan , Lester Lobo , Digamber Shripati Pawar , Nikhil Umesh Mohe , Radhakishnan Venkatasubramanian Tarur
发明人： Divya Lal Saksena , Chandrakesan Muralidharan , Lester Lobo , Digamber Shripati Pawar , Nikhil Umesh Mohe , Radhakishnan Venkatasubramanian Tarur
IPC分类号： A61K38/12 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K14/75 , C07K14/78 , C07K7/06 , A61K38/00
CPC分类号： C07K14/75 , A61K38/00 , C07K7/06 , C07K14/78
摘要： The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.
摘要翻译：本发明涉及使用Fmoc固相合成技术大规模合成环七肽的改进方法。所描述的方法通过肽键彼此偶联在固体支持树脂上组装肽，以获得肽，其中半胱氨酸与树脂的偶联采用溶剂的组合以减少半胱氨酸外消旋化。所描述的方法涉及使用C1-C4醇作为有机腈的总替代物，从而使该方法成本有效，无毒和环保。

2. 发明申请

US20120035117A1 Process for Synthesis of Cyclic Octapeptide 有权
标题翻译：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％。

3. 发明申请

US20110118437A1 Process for the Synthesis of Cyclic Heptapeptide 有权
标题翻译：环肽肽合成方法
公开(公告)号：US20110118437A1
公开(公告)日：2011-05-19
申请号：US13007736
申请日：2011-01-17
申请人： DIVYA LAL SAKSENA , Chandrakesan Muralidharan , Lester Lobo , Digamber Shripati Pawar , NIKHIL UMESH MOHE , Radhakishnan Venkatasubramania Tarur
发明人： DIVYA LAL SAKSENA , Chandrakesan Muralidharan , Lester Lobo , Digamber Shripati Pawar , NIKHIL UMESH MOHE , Radhakishnan Venkatasubramania Tarur
IPC分类号： C07K7/64
CPC分类号： C07K14/75 , A61K38/00 , C07K7/06 , C07K14/78
摘要： The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.
摘要翻译：本发明涉及使用Fmoc固相合成技术大规模合成环七肽的改进方法。所描述的方法通过肽键彼此偶联在固体支持树脂上组装肽，以获得肽，其中半胱氨酸与树脂的偶联采用溶剂的组合以减少半胱氨酸外消旋化。所描述的方法涉及使用C1-C4醇作为有机腈的总替代物，从而使该方法成本有效，无毒和环保。

4. 发明授权

US08377891B2 Process for synthesis of cyclic octapeptide 有权
标题翻译：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％。

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