发明名称 METHODOLOGY FOR PREPARING COMBINATORIAL LIBRARIES BASED UPON A BICYCLIC SCAFFOLD
摘要 The present invention relates to tetrahydro-pyrrolo[1,2-a]imidazole-2,5-dione derivative compounds, hexahydropyrrolo[1,2-a]pyrimidine-2,6-dione derivative compounds, and combinatorial libraries comprising such compounds. The present invention also relates to methods of preparing such compounds. The present invention also relates to methods of preparing such compounds. The methods first involve providing a functionalized resin solid support. Next, the functionalized resin solid support is reacted with amino acids under conditions effective to produce a resin bound dipeptide or tripeptide alcohol intermediate compound. Then, the resin bound dipeptide or tripeptide alcohol intermediate compound is oxidized under conditions effective to convert the resin bound dipeptide or tripeptide alcohol intermediate compound to a resin bound dipeptide or tripeptide aldehyde intermediate compound, Finally, the resin bound dipeptide or tripeptide aldehyde intermediate compound is cyclized under conditions effective to produce the tetrahydro-pyrrolo[1,2-a]imidazole-2,5-dione derivative or hexahydro-pyrrolo[1,2-a]pyrimidine-2,6-dione derivative compound. The methods can be performed in solid phase solid/solution phase, or solution phase.
申请公布号 WO2005056523(A3) 申请公布日期 2006.12.07
申请号 WO2004US40620 申请日期 2004.12.06
申请人 THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK 发明人 HANGAUER, DAVID, G.;AL-ZAHABY, MOHAMED, AYMAN
分类号 C07D209/02;A01N43/42;A61K31/4188;A61K31/675;A61K31/69;C07D;C07D209/04;C07D487/04;G01N33/53 主分类号 C07D209/02
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