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公开(公告)号:US07439222B2
公开(公告)日:2008-10-21
申请号:US11021952
申请日:2004-12-23
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,包括提供包含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,从而将肽片段上的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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2.
公开(公告)号:US06818789B2
公开(公告)日:2004-11-16
申请号:US10364692
申请日:2003-02-10
申请人: Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
发明人: Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
IPC分类号: C07C6966
CPC分类号: C07F3/02 , C07B2200/07 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07C69/716 , C07C69/675
摘要: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
摘要翻译: 本发明涉及用于制备下式的δ-内酯的新方法:使用下式的酰卤:其中R 1,R 2,R 3和X在本文中描述,以及新颖的 中间体。 特别地,本发明涉及对映选择性地制备(R) - 内酯的方法。
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3.
公开(公告)号:US06858749B2
公开(公告)日:2005-02-22
申请号:US10364536
申请日:2003-02-10
申请人: Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
发明人: Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
IPC分类号: C07B61/00 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07F3/02 , C07C69/66
CPC分类号: C07F3/02 , C07B2200/07 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07C69/716 , C07C69/675
摘要: The present invention relates to a novel process for producing a δ-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-δ-lactone.
摘要翻译: 本发明涉及用于制备下式的δ-内酯的新方法:使用下式的酰卤:其中R 1,R 2,R 3和X在本文中描述,以及新颖的 中间体。 特别地,本发明涉及对映选择性地制备(R) - 内酯的方法。
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4.
公开(公告)号:US06545165B1
公开(公告)日:2003-04-08
申请号:US09668834
申请日:2000-09-22
申请人: Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
发明人: Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
IPC分类号: C07D30932
CPC分类号: C07F3/02 , C07B2200/07 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07C69/716 , C07C69/675
摘要: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
摘要翻译: 本发明涉及用于制备下式的δ-内酯的新方法:使用下式的酰卤:其中R1,R2 R3和X如本文所述,以及新的中间体。 特别地,本发明涉及对映选择性地制备(R) - 内酯的方法。
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公开(公告)号:US06743927B2
公开(公告)日:2004-06-01
申请号:US10364547
申请日:2003-02-10
申请人: Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
发明人: Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
IPC分类号: C07D30932
CPC分类号: C07F3/02 , C07B2200/07 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07C69/716 , C07C69/675
摘要: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
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6.
公开(公告)号:US06552204B1
公开(公告)日:2003-04-22
申请号:US09668799
申请日:2000-09-22
IPC分类号: C07F704
CPC分类号: C07D309/32 , C07F7/1804 , Y02P20/55
摘要: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein. In particular, the present invention relates to a process for enantioselectively producing the &dgr;-lactone and novel intermediates disclosed herein.
摘要翻译: 本发明涉及用于制备下式的δ-内酯的新方法:使用下式的酰卤:其中R1,R2 R3和X如本文所述。 特别地,本发明涉及对映选择性地生产本文公开的δ-内酯和新型中间体的方法。
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