公开(公告)号：WO0020357A3

公开(公告)日：2000-10-26

申请号：PCT/GB9903286

申请日：1999-10-05

申请人： GLAXO GROUP LTD ,  CARR ROBIN ARTHUR ELLIS ,  GEHANNE SYLVIE ,  KAY CORINNE ,  MCKEOWN STEPHEN CARL ,  MURRAY PETER JOHN ,  PAIO ALFREDO ,  SCICINSKI JAN JOSEF ,  WATSON STEPHEN PAUL ,  WILLIAMS GEOFFREY MARTYN ,  ZARAMELLA ALESSIO

发明人： CARR ROBIN ARTHUR ELLIS ,  GEHANNE SYLVIE ,  KAY CORINNE ,  MCKEOWN STEPHEN CARL ,  MURRAY PETER JOHN ,  PAIO ALFREDO ,  SCICINSKI JAN JOSEF ,  WATSON STEPHEN PAUL ,  WILLIAMS GEOFFREY MARTYN ,  ZARAMELLA ALESSIO

IPC分类号： G01N27/62 ,  A61K45/00 ,  B01J20/281 ,  C07B61/00 ,  C07C235/20 ,  C07C271/20 ,  C07C311/18 ,  C07D239/42 ,  G01N30/88 ,  G01N33/531 ,  C07C237/18 ,  C07D239/38

CPC分类号： C40B50/16 ,  B01J2219/005 ,  B01J2219/00581 ,  B01J2219/0072 ,  C07B2200/05 ,  C07B2200/11 ,  C07C235/20 ,  C07C311/18 ,  C40B20/08 ,  C40B30/04 ,  C40B40/04 ,  C40B70/00

摘要： The invention provides a chemical construct for use in solid phase synthesis comprising a solid support Q having linked thereto via a connecting group Y a substrate R; the connecting group Y having first and second cleavage sites which are orthogonally and selectively cleavable; the second cleavage site being selectively cleavable to release the substrate; and the first cleavage site being located at a position between the second cleavage site and the solid support and being selectively cleavable to release a fragment Fr comprising the substrate and at least a portion of the connecting group Y; characterised in that cleavage at the first cleavage site forms or introduces on the chemical fragment Fr at the first cleavage site a moiety comprising a sensitising group G (such as an amino group) which sensitises the chemical fragment Fr to instrumental, e.g. mass spectroscopic, analysis. Also provided are methods of analysis employing the constructs, as well as intermediate constructs.

摘要翻译： 本发明提供了用于固相合成的化学构建体，其包括通过连接基团Y与基底R连接的固体支持物Q; 连接基团Y具有正交和可选择性切割的第一和第二切割位点; 第二切割位点是可选择性切割的以释放底物; 并且所述第一切割位点位于所述第二切割位点和所述固体支持物之间的位置，并且可选择性地切割以释放包含所述基底和所述连接基团Y的至少一部分的片段Fr; 其特征在于，第一切割位点处的切割在第一切割位点处的化学片段Fr上形成或引入包含使化学片段Fr致敏的器官的致敏基团G（例如氨基）的部分。 质谱分析。 还提供了使用构建体的分析方法以及中间构建体。