13428-06-3Relevant articles and documents
Generation and reaction of cyano-substituted aryllithium compounds using microreactors
Nagaki, Aiichiro,Kim, Heejin,Usutani, Hirotsugu,Matsuo, Chika,Yoshida, Jun-Ichi
supporting information; experimental part, p. 1212 - 1217 (2010/06/13)
We developed a microflow method for the generation and reactions of aryllithiums bearing a cyano group, including o-lithiobenzonitrile, m-lithiobenzonitrile and p-lithiobenzonitrile. The method was effective at much higher temperatures than are required for conventional macrobatch reactions, by virtue of rapid mixing, short residence time, and efficient temperature control. In addition, reactions of o-lithiobenzonitrile with carbonyl compounds followed by trapping of the resulting lithium alkoxides with electrophiles were achieved in an integrated microflow system. The Royal Society of Chemistry.
Design, synthesis, and structure-activity relationships of pyrazolo[3,4-d]pyrimidines: A novel class of potent enterovirus inhibitors
Chern, Jyh-Haur,Shia, Kak-Shan,Hsu, Tsu-An,Tai, Chia-Liang,Lee, Chung-Chi,Lee, Yen-Chun,Chang, Chih-Shiang,Tseng, Sung-Nien,Shih, Shin-Ru
, p. 2519 - 2525 (2007/10/03)
A series of pyrazolo[3,4-d]pyrimidines were synthesized and their antiviral activity was evaluated in a plaque reduction assay. It is very interesting that this class of compounds provide remarkable evidence that they are very specific for human enteroviruses, in particular, coxsackieviruses. Some derivatives proved to be highly effective in inhibiting enterovirus replication at nanomolar concentrations. SAR studies revealed that the phenyl group at the N-1 position and the hydrophobic diarylmethyl group at the piperazine largely influenced the in vitro antienteroviral activity of this new class of potent antiviral agents. It was found that the pyrazolo[3,4-d]pyrimidines with a thiophene substituent, such as compounds 20-24, in general exhibited high activity against coxsackievirus B3 (IC50=0.063-0.089μM) and moderate activity against enterovirus 71 (IC50=0.32-0.65μM) with no apparent cytotoxic effect toward RD (rhabdomyosarcoma) cell lines (CC5025μ M).
Preparation of highly functionalized Grignard reagents by an iodine-magnesium exchange reaction and its application in solid-phase synthesis
Boymond, Laure,Rottlaender, Mario,Cahiez, Gerard,Knochel, Paul
, p. 1701 - 1703 (2007/10/03)
At -40°C aryl iodides that contain other functional groups can be selectively converted into Grignard reagents, which react with electrophiles such as benzaldehyde in the usual manner [Eq. (a)]. Aryl bromides and iodides that are immobilized as esters on a Wang resin behave analogously.
