1242618-50-3Relevant academic research and scientific papers
An odorless, one-pot synthesis of nitroaryl thioethers via SNAr reactions through the in situ generation of S-alkylisothiouronium salts
Lu, Guo-Ping,Cai, Chun
, p. 59990 - 59996 (2014)
A newly developed C-S bond formation nucleophilic aromatic substitution (SNAr) reaction in aqueous Triton X-100 (TX100) micelles has been disclosed. This chemistry, in which odorless, cheap and stable thiourea in place of thiols is used as the sulfur reagent, provides an efficient approach for the generation of nitroaryl thioethers, which are useful structural units of many bioactive molecules, rendering this methodology attractive to both synthetic and medicinal chemistry.
The invention relates to a thiourea as the sulfur source synthesis of substituted 2 - aryl benzo thiazole
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Paragraph 0019, (2017/08/25)
The invention discloses a method for synthesizing poly-substituted 2-aryl benzothiazoles by utilizing thiourea as a sulphur source. According to the method, thiourea reacts with benzyl chloride to generate an S-benzylisothiourea salt in situ. After that, through the aromatic nucleophilic substitution reaction of the obtained S-benzylisothiourea salt with 2-fluoronitrobenzene and then the one-step reduction (one-pot reaction) process, o-amino phenyl benzyl thioether as an intermediate product can be obtained. Finally, through the iron-catalyzed cross-dehydrogenative-coupling reaction of the o-amino phenyl benzyl thioether, a target product can be obtained. Compared with the traditional synthetic method, the method has the significant advantages of (1) short reaction step, wherein the target product can be synthesized through only three steps of simple reactions by utilizing simple chemical raw materials; (2) mild reaction condition, high atom economy, and relatively safe and cheap reaction reagents; (3) high reaction yield, good substrate tolerance and free of any dangerous or high-toxicity reagent. Therefore, the method might be applied to the large-scale production.
[11C]GSK2126458 and [18F]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers
Wang, Min,Gao, Mingzhang,Miller, Kathy D.,Sledge, George W.,Zheng, Qi-Huang
experimental part, p. 1569 - 1574 (2012/04/04)
GSK2126458 is a highly potent inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with low picomolar to subnanomolar activity. [11C]GSK2126458 and [18F]GSK212 6458, new potential PET agents for imaging of PI3K and mTOR in cancer, were first designed and synthesized in 40-50% and 20-30% decay corrected radiochemical yield, and 370-740 and 37-222 GBq/lmol specific activity at end of bombardment (EOB), respectively.
Synthesis of isomeric fluoronitrobenzene-sulfonyl chlorides
Zhersh, Sergey,Lukin, Oleg,Matvienko, Vitaly,Tolmachev, Andrey
experimental part, p. 5982 - 5986 (2010/10/01)
The synthesis of five hitherto unknown isomeric fluoronitrobenzenesulfonyl chlorides is described. The compounds are prepared from difluoronitrobenzenes by a two-step procedure. In the first step the starting compounds undergo a regioselective reaction with phenylmethanethiol giving rise to the corresponding thioethers. The oxidative cleavage of the latter with chlorine results in the sulfonyl chlorides in good yields. One example of a threefold sequential functionalization of 2-fluoro-6-nitrobenzenesulfonyl chloride showing the synthetic utility of the title compounds is provided.
