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    • 7. 发明授权
      US06566515B1 Photocleavable protecting groups and methods for their use 有权
    • Photocleavable protecting groups and methods for their use
    • 可透光保护组及其使用方法
    • US06566515B1
    • 2003-05-20
    • US09525045
    • 2000-03-14
    • Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
    • Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
    • C07H2104
    • C07H21/00 , B01J2219/00432 , C07B2200/11 , C07H19/10 , C07H19/20 , C07H19/207 , C07K1/061 , C40B40/04 , C40B50/14 , C40B60/14 , G01N33/54353 , Y02P20/55
    • Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Ar—C(R1)(R2)—O—C(O)— wherein: Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof; R1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; and X is a leaving group, a chemical fragment linked to Ar—C(R1)(R2)—O—C(O)— via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R1 and R2 are H, X is not linked to Ar—C(R1)(R2)—O—C(O)— via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R1 and R2 are electron donating groups. A particularly preferred protecting group is the “PYMOC” protecting group, pyrenylmethyloxycarbonyl, where Ar is pyrenyl and R1 and R2 are H. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
    • 提供了新的化合物，其可用作化学合成中的连接基团，优选在寡核苷酸和多肽的固相合成中。 这些化合物通常是光不稳定的并且包括可以通过光解去除以揭示反应性基团的保护基团。 保护基具有通式Ar-C（R 1）（R 2）-OC（O） - ，其中：Ar是任选取代的稠合多环芳基或杂芳族基团或其杂原子衍生物; R 1和R 2独立地是H， 烷基，烯基或炔基，任选取代的芳基或任选取代的杂芳族，或前述的维果衍生物; 和X是离去基团，通过杂原子与固体载体连接至Ar-C（R 1）（R 2）-O-C（O） - 的化学片段; 条件是当Ar为1-芘基且R 1和R 2为H时，X不能通过氮原子与Ar-C（R 1）（R 2）-O-C（O） - 连接。 优选的实施方案是其中Ar是稠合多环芳烃并且其中Ar，R 1和R 2上的取代基是给电子基团的实施方案。 特别优选的保护基是“PYMOC”保护基团，芘基甲氧基羰基，其中Ar是芘基，R 1和R 2是H.另外提供了一种从成分分子在载体上形成多种化合物的方法， 使用上述保护的化合物分离预定区域的载体。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      US20100280234A1 Photocleavable Protecting Groups and Methods for Their Use 审中-公开
    • Photocleavable Protecting Groups and Methods for Their Use
    • 可剥离保护组及其使用方法
    • US20100280234A1
    • 2010-11-04
    • US12343782
    • 2008-12-24
    • Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
    • Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
    • C07H19/10
    • C07H21/00 , B01J2219/00432 , C07B2200/11 , C07H19/10 , C07H19/20 , C07H19/207 , C07K1/061 , C40B40/04 , C40B50/14 , C40B60/14 , G01N33/54353 , Y02P20/55
    • Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Ar—C(R1)(R2)—O—C(O)— wherein: Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof; R1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; and X is a leaving group, a chemical fragment linked to Ar—C(R1)(R2)—O—C(O)— via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R1 and R2 are H, X is not linked to Ar—C(R1)(R2)—O—C(O)— via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R1 and R2 are electron donating groups. A particularly preferred protecting group is the “PYMOC” protecting group, pyrenylmethyloxycarbonyl, where Ar is pyrenyl and R1 and R2 are H. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
    • 提供了新的化合物，其可用作化学合成中的连接基团，优选在寡核苷酸和多肽的固相合成中。 这些化合物通常是光不稳定的并且包括可以通过光解去除以揭示反应性基团的保护基团。 保护基具有通式Ar-C（R 1）（R 2）-O-C（O） - ，其中：Ar是任选取代的稠合多环芳基或杂芳族基团或其杂原子衍生物; R 1和R 2独立地为H，任选取代的烷基，烯基或炔基，任选取代的芳基或任选取代的杂芳族化合物，或前述的乙烯衍生物; X是离去基团，经由杂原子连接到Ar-C（R 1）（R 2）-O-C（O） - 或固体载体上的化学片段; 条件是当Ar为1-芘基且R 1和R 2为H时，X不能通过氮原子与Ar-C（R 1）（R 2）-O-C（O） - 连接。 优选的实施方案是其中Ar是稠合多环芳烃并且其中Ar，R 1和R 2上的取代基是给电子基团的实施方案。 特别优选的保护基是“PYMOC”保护基，芘基甲氧基羰基，其中Ar是芘基，R 1和R 2是H.还提供了一种从组分分子在载体上形成多种化合物的方法，每种化合物占据 使用上述保护的化合物分离预定区域的载体。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US07470783B2 Photocleavable protecting groups and methods for their use 有权
    • Photocleavable protecting groups and methods for their use
    • 可透光保护组及其使用方法
    • US07470783B2
    • 2008-12-30
    • US11105571
    • 2005-04-14
    • Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
    • Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
    • C07H21/00
    • C07H21/00 , B01J2219/00432 , C07B2200/11 , C07H19/10 , C07H19/20 , C07H19/207 , C07K1/061 , C40B40/04 , C40B50/14 , C40B60/14 , G01N33/54353 , Y02P20/55
    • Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Ar—C(R1)(R2)—O—C(O)-wherein: Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof; R1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; and X is a leaving group, a chemical fragment linked to Ar—C(R1)(R2)—O—C(O)— via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R1 and R2 are H, X is not linked to Ar—C(R1)(R2)—O—C(O)— via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R1 and R2 are electron donating groups. A particularly preferred protecting group is the “PYMOC” protecting group, pyrenylmethyloxycarbonyl, where Ar is pyrenyl and R1 and R2 are H. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
    • 提供了新的化合物，其可用作化学合成中的连接基团，优选在寡核苷酸和多肽的固相合成中。 这些化合物通常是光不稳定的并且包括可以通过光解去除以揭示反应性基团的保护基团。 保护基具有通式Ar-C（R 1）（R 2）-O-C（O） - ，其中：Ar是任选取代的稠合多环芳基或杂芳族基团或其杂原子衍生物; R 1和R 2独立地为H，任选取代的烷基，烯基或炔基，任选取代的芳基或任选取代的杂芳族化合物，或前述的乙烯衍生物; X是离去基团，经由杂原子连接到Ar-C（R 1）（R 2）-O-C（O） - 或固体载体上的化学片段; 条件是当Ar为1-芘基且R 1和R 2为H时，X不能通过氮原子与Ar-C（R 1）（R 2）-O-C（O） - 连接。 优选的实施方案是其中Ar是稠合多环芳烃并且其中Ar，R 1和R 2上的取代基是给电子基团的实施方案。 特别优选的保护基是“PYMOC”保护基，芘基甲氧基羰基，其中Ar是芘基，R 1和R 2是H.还提供了一种从组分分子在载体上形成多种化合物的方法，每种化合物占据 使用上述保护的化合物分离预定区域的载体。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      US06881836B2 Photocleavable protecting groups and methods for their use 失效
    • Photocleavable protecting groups and methods for their use
    • 可透光保护组及其使用方法
    • US06881836B2
    • 2005-04-19
    • US10348917
    • 2003-01-22
    • Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
    • Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
    • B05D3/00 , C07B61/00 , C07H19/10 , C07H19/20 , C07H19/207 , C07H21/00 , C07K1/06 , C40B60/14 , G01N33/543
    • C07H21/00 , B01J2219/00432 , C07B2200/11 , C07H19/10 , C07H19/20 , C07H19/207 , C07K1/061 , C40B40/04 , C40B50/14 , C40B60/14 , G01N33/54353 , Y02P20/55
    • Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Ar—C(R1)(R2)—O—C(O)— wherein: Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof; R1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; and X is a leaving group, a chemical fragment linked to Ar—C(R1)(R2)—O—C(O)— via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R1 and R2 are H, X is not linked to Ar—C(R1)(R2)—O—C(O)— via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R1 and R2 are electron donating groups. A particularly preferred protecting group is the “PYMOC” protecting group, pyrenylmethyloxycarbonyl, where Ar is pyrenyl and R1 and R2 are H. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
    • 提供了新的化合物，其可用作化学合成中的连接基团，优选在寡核苷酸和多肽的固相合成中。 这些化合物通常是光不稳定的并且包括可以通过光解去除以揭示反应性基团的保护基团。 保护基具有通式Ar-C（R 1）（R 2） - OC（O） - ，其中：Ar是任选取代的稠合多环芳基或杂芳族 组或其衍生物; R 1和R 2独立地为H，任选取代的烷基，烯基或炔基，任选取代的芳基或任选取代的杂芳族，或前述的维果衍生物; X是离去基团，经由杂原子与Ar-C（R 1）（R 2）-O（O） - 连接的化学片段或固体 支持; 条件是当Ar为1-芘基且R 1和R 2为H时，X不与Ar-C（R 1） （R 2）-O（O） - 经由氮原子。 优选的实施方案是其中Ar是稠合多环芳烃并且其中Ar 1，R 1和R 2上的取代基是给电子基团的实施方案。 特别优选的保护基是“PYMOC”保护基，芘基甲氧基羰基，其中Ar是芘基，R 1和R 2都是H.还提供了一种形成， 使用上述保护的化合物，从成分分子，载体上的多种化合物，每种化合物占据支持体的单独的预定区域。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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