Design and synthesis of dihydroisoquinolones for fragment-based drug discovery (FBDD). Issue 5 (7th January 2016)

• Record Type: Journal Article
• Authors: Palmer, Nick; Peakman, Torren M.; Norton, David; Rees, David C.
• Is Part Of: Organic & biomolecular chemistry. Volume 14:Issue 5(2016)
• Page Start: 1599
• Page End: 1610
• Publication Date: 2016-01-07
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c5ob02461g
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : FBDD creates new opportunities for synthetic chemistry. Abstract : This study describes general synthesis aspects of fragments for FBDD, as illustrated by the dihydroisoquinolones1–3 . 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.