Design and synthesis of dihydroisoquinolones for fragment-based drug discovery (FBDD)

This study describes general synthesis aspects of fragments for FBDD, as illustrated by the dihydroisoquinolones 1-3 . Previous Rh( iii ) methodology is extended to incorporate amines, heteroatoms (N and S), and substituents (halogen, ester) as potential binding groups and/or synthetic growth points...

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Bibliographic Details
Published in:Organic & biomolecular chemistry 2016-02, Vol.14 (5), p.1599-161
Main Authors: Palmer, Nick, Peakman, Torren M, Norton, David, Rees, David C
Format: Article
Language:English
Subjects:
Drug Design
Drug Discovery
Isoquinolines - chemical synthesis
Isoquinolines - chemistry
Molecular Structure
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Summary:This study describes general synthesis aspects of fragments for FBDD, as illustrated by the dihydroisoquinolones 1-3 . Previous Rh( iii ) methodology is extended to incorporate amines, heteroatoms (N and S), and substituents (halogen, ester) as potential binding groups and/or synthetic growth points for fragment-to-lead elaboration. FBDD creates new opportunities for synthetic chemistry.
ISSN:1477-0520
1477-0539
DOI:10.1039/c5ob02461g