1242653-17-3Relevant academic research and scientific papers
Synthesis, biological evaluation, and structure-activity relationships of tri- and tetrasubstituted olefins related to isocombretastatin A-4 as new tubulin inhibitors
Aziz, Jessy,Brachet, Etienne,Hamze, Abdallah,Peyrat, Jean-Fran?ois,Bernadat, Guillaume,Morvan, Estelle,Bignon, Jér?me,Wdzieczak-Bakala, Joanna,Desravines, Déborah,Dubois, Joelle,Tueni, Marie,Yassine, Ahmad,Brion, Jean-Daniel,Alami, Mouad
, p. 430 - 442 (2013/02/23)
The synthesis and structure-activity relationships associated with a series of 1,1-diarylethylene tubulin polymerization inhibitors 3 and 4 are described. The key step for their preparation involves a palladium-catalyzed coupling of N-arylsulfonylhydrazon
Pd-catalyzed reaction of sterically hindered hydrazones with aryl halides: Synthesis of tetra-substituted olefins related to iso-combretastatin A4
Brachet, Etienne,Hamze, Abdallah,Peyrat, Jean-Francois,Brion, Jean-Daniel,Alami, Mouad
supporting information; experimental part, p. 4042 - 4045 (2010/11/16)
PdCl2(MeCN)2 in combination with dppp proved to be a powerful and efficient catalyst for the coupling of sterically hindered N-arylsulfonylhydrazones with aryl halides, thus providing a flexible and convergent access to tetrasubstituted olefins related to iso-combretastatin A4 in good yields. This new protocol has been applied successfully to the formal synthesis of biphenylisopropylidene 4-pyridine CYP17 inhibitor, 12b, of biological interest.
