title: Design and synthesis of dihydroisoquinolones for fragment-based drug discovery (FBDD).
abstract: 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.
authors.affiliation: Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, UK. david.rees@astx.com.
authors.forename: Nick
authors.initials: N
authors.lastname: Palmer
authors.affiliation: Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, UK. david.rees@astx.com.
authors.forename: Torren M
authors.initials: TM
authors.lastname: Peakman
authors.affiliation: Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, UK. david.rees@astx.com.
authors.forename: David
authors.initials: D
authors.lastname: Norton
authors.affiliation: Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, UK. david.rees@astx.com.
authors.forename: David C
authors.initials: DC
authors.lastname: Rees
mesh_terms: D015195:Drug Design; D055808:Drug Discovery; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure
chemical_list: D007546:Isoquinolines