| Autor: |
Zhang L; Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, Kansas 66045, USA., Lushington GH, Neuenswander B, Hershberger JC, Malinakova HC |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of combinatorial chemistry [J Comb Chem] 2008 Mar-Apr; Vol. 10 (2), pp. 285-302. Date of Electronic Publication: 2008 Feb 01. |
| DOI: |
10.1021/cc700151m |
| Abstrakt: |
Parallel solution-phase synthesis of combinatorial libraries of hexahydro-1 H-isoindolones exploiting a novel "tactical combination" of Cu-catalyzed three-component coupling and Diels-Alder reactions was accomplished. Three distinct libraries consisting of 24 members (library I), 60 members (library II), and 32 members (library III) were constructed. Variation of three substituents on the isoindolone scaffold in library I was exclusively achieved by the choice of the building blocks. In the syntheses of libraries II and III, sublibraries of isoindolone scaffolds were prepared initially in a one-pot/two-step process and were further diversified via Pd-catalyzed Suzuki cross-coupling reaction with boronic acids at two different diversification points. The Lipinski profiles and calculated ADME properties of the compounds are also reported. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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