公开(公告)号：EP1119529B1

公开(公告)日：2003-09-17

申请号：EP99947750.8

申请日：1999-10-05

申请人： GLAXO GROUP LIMITED

发明人： CARR, Robin, Arthur, Ellis c/o Glaxo Wellcome plc ,  GEHANNE, Sylvie Glaxo Wellcome SpA ,  KAY, Corinne c/o Glaxo Wellcome Chemistry Lab. ,  McKEOWN, Stephen, Carl Glaxo Wellcome plc ,  MURRAY, Peter, John OSI Pharmaceuticals ,  PAIO, Alfredo Glaxo Wellcome SpA ,  SCICINSKI, Jan c/o Glaxo Wellcome Chemistry Lab. ,  WATSON, Stephen, Paul Glaxo Wellcome plc ,  WILLIAMS, G. c/o Glaxo Wellcome Chemistry Lab. ,  ZARAMELLA, Alessio Glaxo Wellcome SpA

IPC分类号： C07B61/00 ,  C07D239/38 ,  C07C271/20 ,  C07C311/18 ,  C07C237/18

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.