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1. 发明申请

WO2008077799A2 COMPOUNDS AND METHODS FOR AMINO-ALKYLENEDIOL SYNTHESIS 审中-公开
标题翻译：氨基亚氨基二醇合成的化合物和方法
公开(公告)号：WO2008077799A2
公开(公告)日：2008-07-03
申请号：PCT/EP2007/063835
申请日：2007-12-12
申请人： F. HOFFMANN-LA ROCHE AG , CAIN, Robert O. , MOORLAG, Hendrick , TUCKER, Charles E. , WONG, Jim-Wah
发明人： CAIN, Robert O. , MOORLAG, Hendrick , TUCKER, Charles E. , WONG, Jim-Wah
IPC分类号： C07C213/02 , C07C215/10 , C07C215/20 , C07C215/40 , C07C215/42
CPC分类号： C07C213/02 , C07C215/16 , Y02P20/55 , C07C215/10
摘要： A method of making an amino-alkylenediol and intermediate compounds useful in the method is disclosed. The method includes preparing a first intermediate compound comprising an aminoalkylene diol wherein a protecting group is linked to the amino functionality, and optionally, preparing a second intermediate compound comprising a salt of the first intermediate compound. The first intermediate compound has the structure of Formula (II ) wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, and Z is a protecting group. The second intermediate compound has the structure of Formula (III ) wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, TsO - is toluene sulfonate, and Z is a protecting group.
摘要翻译：公开了制备在该方法中有用的氨基亚烷基二醇和中间体化合物的方法。该方法包括制备包含氨基亚烷基二醇的第一中间体化合物，其中保护基与氨基官能团连接，以及任选地制备包含第一中间体化合物的盐的第二中间体化合物。第一中间体化合物具有式（II）的结构，其中R是具有2至20个碳原子的二价亚烷基，X和Y独立地是二价连接部分或单键，Z是保护基。第二中间体化合物具有式（III）的结构，其中R是具有2至20个碳原子的二价亚烷基，X和Y独立地是二价连接部分或单键，TsO-是甲苯磺酸盐，Z是一个保护组。

2. 发明申请

WO2008077799A3 COMPOUNDS AND METHODS FOR AMINO-ALKYLENEDIOL SYNTHESIS 审中-公开
标题翻译：氨基 - 烷基二醇合成的化合物和方法
公开(公告)号：WO2008077799A3
公开(公告)日：2008-08-14
申请号：PCT/EP2007063835
申请日：2007-12-12
申请人： HOFFMANN LA ROCHE , CAIN ROBERT O , MOORLAG HENDRICK , TUCKER CHARLES E , WONG JIM-WAH
发明人： CAIN ROBERT O , MOORLAG HENDRICK , TUCKER CHARLES E , WONG JIM-WAH
IPC分类号： C07C213/02 , C07C215/10 , C07C215/20 , C07C215/40 , C07C215/42
CPC分类号： C07C213/02 , C07C215/16 , Y02P20/55 , C07C215/10
摘要： A method of making an amino-alkylenediol and intermediate compounds useful in the method is disclosed. The method includes preparing a first intermediate compound comprising an aminoalkylene diol wherein a protecting group is linked to the amino functionality, and optionally, preparing a second intermediate compound comprising a salt of the first intermediate compound. The first intermediate compound has the structure of Formula (II ) wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, and Z is a protecting group. The second intermediate compound has the structure of Formula (III ) wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, TsO - is toluene sulfonate, and Z is a protecting group.
摘要翻译：公开了一种制备氨基亚烷基二醇的方法和用于该方法的中间体化合物。该方法包括制备包含氨基亚烷基二醇的第一中间体化合物，其中保护基与氨基官能团连接，并且任选地制备包含第一中间体化合物的盐的第二中间体化合物。第一中间体化合物具有式（II）的结构，其中R为具有2至20个碳原子的二价亚烷基，X和Y独立地为二价连接部分或单键，并且Z为保护基。第二中间体化合物具有式（III）的结构，其中R为具有2至20个碳原子的二价亚烷基，X和Y独立地为二价连接部分或单键，TsO-为甲苯磺酸盐，并且Z为一个保护组。

3. 发明申请

WO2005063791B1 PROCESS FOR PEPTIDE SYNTHESIS USING A REDUCED AMOUNT OF DEPROTECTION AGENT 审中-公开
标题翻译：使用减少剂量的保护剂进行肽合成的方法
公开(公告)号：WO2005063791B1
公开(公告)日：2005-11-10
申请号：PCT/EP2004014599
申请日：2004-12-22
申请人： HOFFMANN LA ROCHE , GUINN MARTIN R , HODGES LEWIS M , JOHNSTON DAVID A , MOORLAG HENDRICK , SCHWINDT MARK A
发明人： GUINN MARTIN R , HODGES LEWIS M , JOHNSTON DAVID A , MOORLAG HENDRICK , SCHWINDT MARK A
IPC分类号： C07K1/02 , C07K1/04
CPC分类号： C07K1/04 , C07K1/026 , Y02P20/55
摘要： The invention provides methods of synthesizing peptides, involving the steps of providing a composition including a peptide fragment, wherein the peptide fragment has at least one amino acid residue and includes a base-sensitive, N-terminal protecting group; removing the base-sensitive, N-terminal protecting group from the peptide fragment using a deprotection reagent that includes a base, whereby an N-terminal functionality on the peptide fragment is deprotected; removing the base from the composition to provide a residual base content of more than 100 ppm; causing a reactive peptide fragment having a reactive C-terminus and a base-sensitive N-terminal protecting group to react with the deprotected N-terminal functionality of the peptide fragment under conditions such that the reactive peptide fragment is added to the peptide fragment; and optionally repeating the deprotection and coupling steps until a desired peptide is obtained. Also provided are methods of synthesizing peptides, wherein base is removed from the composition to a point where the composition would provide a positive chloranil test. Also provided are methods of synthesizing peptides, wherein coupling is performed in basic reaction mixtures.
摘要翻译：本发明提供了合成肽的方法，包括提供包括肽片段的组合物的步骤，其中肽片段具有至少一个氨基酸残基并且包括碱敏感的N-末端保护基; 使用包含碱的去保护试剂从肽片段中除去碱敏感的N-末端保护基，由此将肽片段上的N-末端官能团去保护; 从组合物中除去碱以提供大于100ppm的残留碱含量; 使得具有反应性C末端和碱敏感性N末端保护基团的反应性肽片段与肽片段的去保护的N末端官能团反应，使得将反应性肽片段加入到肽片段中; 并任选地重复脱保护和偶联步骤，直至获得所需的肽。还提供了合成肽的方法，其中将碱从组合物中除去至组合物将提供正氯醌测试的程度。还提供了合成肽的方法，其中在碱性反应混合物中进行偶联。

4. 发明申请

WO2005063791A3 PROCESS FOR PEPTIDE SYNTHESIS USING A REDUCED AMOUNT OF DEPROTECTION AGENT 审中-公开
公开(公告)号：WO2005063791A3
公开(公告)日：2005-07-14
申请号：PCT/EP2004/014599
申请日：2004-12-22
申请人： F.HOFFMANN-LA ROCHE AG , GUINN, Martin, R. , HODGES, Lewis, M. , JOHNSTON, David, A. , MOORLAG, Hendrick , SCHWINDT, Mark, A.
发明人： GUINN, Martin, R. , HODGES, Lewis, M. , JOHNSTON, David, A. , MOORLAG, Hendrick , SCHWINDT, Mark, A.
IPC分类号： C07K1/02
摘要： The invention provides methods of synthesizing peptides, involving the steps of providing a composition including a peptide fragment, wherein the peptide fragment has at least one amino acid residue and includes a base-sensitive, N-terminal protecting group; removing the base-sensitive, N-terminal protecting group from the peptide fragment using a deprotection reagent that includes a base, whereby an N-terminal functionality on the peptide fragment is deprotected; removing the base from the composition to provide a residual base content of more than 100 ppm; causing a reactive peptide fragment having a reactive C-terminus and a base-sensitive N-terminal protecting group to react with the deprotected N-terminal functionality of the peptide fragment under conditions such that the reactive peptide fragment is added to the peptide fragment; and optionally repeating the deprotection and coupling steps until a desired peptide is obtained. Also provided are methods of synthesizing peptides, wherein base is removed from the composition to a point where the composition would provide a positive chloranil test. Also provided are methods of synthesizing peptides, wherein coupling is performed in basic reaction mixtures.

5. 发明申请

WO2005063791A2 PROCESS AND SYSTEMS FOR PEPTIDE SYNTHESIS 审中-公开
标题翻译：肽合成的方法和系统
公开(公告)号：WO2005063791A2
公开(公告)日：2005-07-14
申请号：PCT/EP2004014599
申请日：2004-12-22
申请人： HOFFMANN LA ROCHE , GUINN MARTIN R , HODGES LEWIS M , JOHNSTON DAVID A , MOORLAG HENDRICK , SCHWINDT MARK A
发明人： GUINN MARTIN R , HODGES LEWIS M , JOHNSTON DAVID A , MOORLAG HENDRICK , SCHWINDT MARK A
IPC分类号： C07K1/02 , C07K1/04 , C07K1/00
CPC分类号： C07K1/04 , C07K1/026 , Y02P20/55
摘要： The invention provides methods of synthesizing peptides, involving the steps of providing a composition including a peptide fragment, wherein the peptide fragment has at least one amino acid residue and includes a base-sensitive, N-terminal protecting group; removing the base-sensitive, N-terminal protecting group from the peptide fragment using a deprotection reagent that includes a base, whereby an N-terminal functionality on the peptide fragment is deprotected; removing the base from the composition to provide a residual base content of more than 100 ppm; causing a reactive peptide fragment having a reactive C-terminus and a base-sensitive N-terminal protecting group to react with the deprotected N-terminal functionality of the peptide fragment under conditions such that the reactive peptide fragment is added to the peptide fragment; and optionally repeating the deprotection and coupling steps until a desired peptide is obtained. Also provided are methods of synthesizing peptides, wherein base is removed from the composition to a point where the composition would provide a positive chloranil test. Also provided are methods of synthesizing peptides, wherein coupling is performed in basic reaction mixtures.
摘要翻译：本发明提供了合成肽的方法，包括提供包括肽片段的组合物的步骤，其中肽片段具有至少一个氨基酸残基并且包括碱敏感的N-末端保护基; 使用包含碱的去保护试剂从肽片段中除去碱敏感的N-末端保护基，由此将肽片段上的N-末端官能团去保护; 从组合物中除去碱以提供大于100ppm的残留碱含量; 使得具有反应性C末端和碱敏感性N末端保护基团的反应性肽片段与肽片段的去保护的N末端官能团反应，使得将反应性肽片段加入到肽片段中; 并任选地重复脱保护和偶联步骤，直至获得所需的肽。还提供了合成肽的方法，其中将碱从组合物中除去至组合物将提供正氯醌测试的程度。还提供了合成肽的方法，其中在碱性反应混合物中进行偶联。

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