专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
参考标题:C-Glycosyl Tyrosines. Synthesis And Incorporation Into C-Glycopeptides 作者:Alan J. Pearce,Sharn Ramaya,Simon N. Thorn,Graham B. Bloomberg,Daryl S. Walter,Timothy Gallagher |发布日期:1999.7.1 摘要:The Synthesis Of The Fmoc-Protected C-Glycosyl Tyrosines 1 And 2, Together With Two Other Related C-Glycosyl Tyrosines, Has Been Achieved. Key Reactions Involved (I) The Reaction Of A Glycal With An Organozinc Reagent (Carrying An Aryl Iodide Function) In The Presence Of A Lewis Acid To Establish The C-Glycosyl Linkage And (II) Subsequent Cross Coupling Of The Aryl Iodide To An Alanyl Zinc Reagent
合成参考文献
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 647.