31082-10-7Relevant academic research and scientific papers
A simple and efficient copper oxide-catalyzed Barbier-Grignard reaction of unactivated aryl or alkyl bromides with ester
Gao, Fei,Deng, Xiang-Jun,Tang, Yu,Tang, Jin-Peng,Yang, Jun,Zhang, Yuan-Ming
supporting information, p. 880 - 883 (2014/02/14)
An efficient one-pot route to synthesize tertiary alcohol compounds using Barbier-Grignard reaction of unactivated alkyl or aryl bromides with ester in THF at 65 C catalyzed by CuO has been developed and systematically investigated. A wide range of substituted tertiary alcohol compounds were obtained in good to high yields. The reaction is highly chemoselective. The mechanism involving the leaving group of R2O-group is discussed.
A simple and efficient copper oxide-catalyzed Barbier-Grignard reaction of unactivated aryl or alkyl bromides with ester
Gao, Fei,Deng, Xiang-Jun,Tang, Yu,Tang, Jin-Peng,Yang, Jun,Zhang, Yuan-Ming
supporting information, p. 880 - 883 (2015/03/03)
An efficient one-pot route to synthesize tertiary alcohol compounds using Barbier-Grignard reaction of unactivated alkyl or aryl bromides with ester in THF at 65 °C catalyzed by CuO has been developed and systematically investigated. A wide range of substituted tertiary alcohol compounds were obtained in good to high yields. The reaction is highly chemoselective. The mechanism involving the leaving group of R2O-group is discussed.
Doing the methylene shuffle - Further insights into the inhibition of mitotic kinesin Eg5 with S-trityl l-cysteine
Abualhasan, Murad N.,Good, James A.D.,Wittayanarakul, Kitiyaporn,Anthony, Nahoum G.,Berretta, Giacomo,Rath, Oliver,Kozielski, Frank,Sutcliffe, Oliver B.,MacKay, Simon P.
experimental part, p. 483 - 498 (2012/09/10)
S-Trityl l-cysteine (STLC) is an inhibitor of the mitotic kinesin Eg5 with potential as an antimitotic chemotherapeutic agent. We previously reported the crystal structure of the ligand-protein complex, and now for the first time, have quantified the interactions using a molecular dynamics based approach. Based on these data, we have explored the SAR of the trityl head group using the methylene shuffle strategy to expand the occupation of one of the hydrophobic pockets. The most potent compounds exhibit strong (100 nM) inhibition of Eg5 in the basal ATPase assay and inhibit growth in a variety of tumour-derived cell lines.
