827031-83-4Relevant articles and documents
Efficient N-arylation of 4-chloroquinazolines en route to novel 4-anilinoquinazolines as potential anticancer agents
Clososki, Giuliano C.,Costa-Lotufo, Leticia V.,Dos Santos, Thiago,Furtado, Luciana C.,Murie, Valter E.,Nishimura, Rodolfo H. V.
supporting information, p. 2968 - 2975 (2022/01/12)
Microwave-mediated N-arylation of 4-chloroquinazolines in THF/H2O rapidly and efficiently afforded a library of novel 6-halo-2- phenyl-substituted 4-anilinoquinazolines. The methodology was compatible with numerous ortho-, meta-, and para-substituted N-methylanilines as well as substituted anilines and furnished the corresponding 4-anilinoquinazolines in good yields. Preliminary screening of the synthesized compounds against tumor cells (HCT-116 and T98G) showed promising antiproliferative properties.
Radiosynthesis and in Vivo Evaluation of [11C]MPC-6827, the First Brain Penetrant Microtubule PET Ligand
Kumar, J. S. Dileep,Solingapuram Sai, Kiran Kumar,Prabhakaran, Jaya,Oufkir, Hakeem R.,Ramanathan, Gayathri,Whitlow, Christopher T.,Dileep, Hima,Mintz, Akiva,Mann, J. John
, p. 2118 - 2123 (2018/03/21)
Abnormalities of microtubules (MTs) are implicated in the pathogenesis of many CNS diseases. Despite the potential of an MT imaging agents, no PET ligand is currently available for in vivo imaging of MTs in the brain. We radiolabeled [11C]MPC-6
Microwave-accelerated Dimroth rearrangement for the synthesis of 4-anilino-6-nitroquinazolines. Application to an efficient synthesis of a microtubule destabilizing agent
Foucourt, Alicia,Dubouilh-Benard, Carole,Chosson, Elizabeth,Corbière, Cécile,Buquet, Catherine,Iannelli, Mauro,Leblond, Bertrand,Marsais, Francis,Besson, Thierry
scheme or table, p. 4495 - 4502 (2010/07/08)
A useful and rapid access to 4-anilino-6-nitroquinazolines was investigated in a multi-gram scale via microwave-accelerated condensation and Dimroth rearrangement of the starting anilines with imines obtained by reaction of anthranilonitriles with formamide dimethylacetal. A novel short and efficient route to Azixa (EPi28495, MPC-6827), a microtubule destabilizing agent and apoptosis inducer, was performed with success demonstrating that well controlled parameters offer comfortable using of microwave technology with safe and environmental benefits.