1427180-45-7Relevant articles and documents
Design and synthesis of dihydroisoquinolones for fragment-based drug discovery (FBDD)
Palmer, Nick,Peakman, Torren M.,Norton, David,Rees, David C.
, p. 1599 - 1610 (2016/02/10)
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.
Complementary regioselectivity in Rh(III)-catalyzed insertions of potassium vinyltrifluoroborate via C-H activation: Preparation and use of 4-trifluoroboratotetrahydroisoquinolones
Presset, Marc,Oehlrich, Daniel,Rombouts, Frederik,Molander, Gary A.
, p. 1528 - 1531 (2013/06/27)
Potassium vinyltrifluoroborate was found to be an efficient partner with benzamide derivatives for Rh(III)-catalyzed annulations. 4- Trifluoroboratotetrahydroisoquinolones were generated under mild conditions, affording a regioisomerically complementary substitution pattern to other alkenes in related reactions. These new boron-containing building blocks were derivatized by N-arylations, retaining the boron substituent for further elaboration.