88373-27-7Relevant articles and documents
Palladium-Catalyzed gem-Difluoroallylation Reaction between Aryltributyltin and Bromodifluoromethylated Alkenes
Chen, Chuan-Xin,Chen, Xiao-Qu,Lu, Heng,Shi, Chang-Yun,Wang, Dong-Yu,Zeng, Ruoqing,Zhang, Ao
supporting information, (2022/02/10)
A robust Stille gem-difluoroallylation of arylstannanes with 3-bromo-3,3-difluoropropenes has been established. The catalyst was found to exert critical effect on the reaction chemoselectivity. By using Pd(OH)2/C as the catalyst, a series of 3-(hetero)ary
Stannylation of Aryl Halides, Stille Cross-Coupling, and One-Pot, Two-Step Stannylation/Stille Cross-Coupling Reactions under Solvent-Free Conditions
Gribanov, Pavel S.,Golenko, Yulia D.,Topchiy, Maxim A.,Minaeva, Lidiya I.,Asachenko, Andrey F.,Nechaev, Mikhail S.
supporting information, p. 120 - 125 (2018/01/17)
Solvent-free protocols for palladium-catalyzed stannylation of aryl halides, Stille cross-coupling, and one-pot, two-step stannylation/Stille cross-coupling (SSC) are reported for the first time. (Het)aryl halides bearing acceptor, donor, as well as sterically demanding substituents are stannylated and/or coupled in high yields. The reactions are catalyzed by conventional palladium(II) acetate/PCy3 [Pd(OAc)2/PCy3] under air, using available base CsF, and without the use of high purity reagents. The developed synthetic procedures are versatile, robust, and easily scalable. The absence of solvent, and the elimination of isolation procedures of aryl stannanes makes the SSC protocol simple, step economical, and highly efficient for the synthesis of biaryls in a one-pot two-step procedure.
Imatinib analogs as potential agents for PET imaging of Bcr-Abl and c-KIT expression at a kinase level
Peng, Zhenghong,Maxwell, David S.,Sun, Duoli,Bhanu Prasad, Basvoju A.,Pal, Ashutosh,Wang, Shimei,Balatoni, Julius,Ghosh, Pradip,Lim, Seok T.,Volgin, Andrei,Shavrin, Aleksander,Alauddin, Mian M.,Gelovani, Juri G.,Bornmann, William G.
, p. 623 - 632 (2014/01/17)
We synthesized two series of imatinib mesylate (STI-571) analogs to develop a Bcr-Abl and c-KIT receptor-specific labeling agent for positron emission tomography (PET) imaging to measure Bcr-Abl and c-KIT expression levels in a mouse model. The methods of molecular modeling, synthesis of STI-571 and its analogs, in vitro kinase assays, and radiolabeling are described. Molecular modeling revealed that these analogs bind the same Bcr-Abl and c-KIT binding sites as those bound by STI-571. The analogs potently inhibit the tyrosine kinase activity of Bcr-Abl and c-KIT, similarly to STI-571. [ 18F]-labeled STI-571 was prepared with high specific activity (75 GBq/μmol) by nucleophilic displacement and an average radiochemical yield of 12%. [131I]-labeled STI-571 was prepared with high purity (>95%) and an average radiochemical yield of 23%. The uptake rates of [ 18F]-STI-571 in K562 cells expressing Abl and in U87WT cells overexpressing c-KIT were significantly higher than those in the U87 cell and could be inhibited by STI-71 (confirming the specificity of uptake). PET scans of K562 and U87WT tumor-bearing mice with [18F]-STI-571 as a contrast agent showed visible tumor uptake and tumor-to-non-target contrast.
FLUORINATION OF ORGANIC COMPOUNDS
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Page/Page column 34, (2010/07/10)
Methods for fluorinating organic compounds are described herein.
New and simple one-step cobalt-catalyzed preparation of functionalized arylstannanes from the corresponding aryl bromides or iodides
Gosmini, Corinne,Perichon, Jacques
, p. 216 - 217 (2007/10/03)
The process for the preparation of functionalized arylstannanes from the corresponding aryl bromides or iodides was described. The corresponding arylstannane was detected by gas chromatography using an internal standard alkane. The two-step coupling react
Photoinduced energy transfer in associated but noncovalently linked photosynthetic model systems
Sessler, Jonathan L.,Wang, Bing,Harriman, Anthony
, p. 704 - 714 (2007/10/02)
The synthesis and photophysical characterization of nucleobase-substituted porphyrins designed to form rigid hydrogen-bonded ensembles, and to allow for energy transfer within the resulting complexes, is reported. Watson-Crick nucleobase-pairing interacti
