1006-20-8Relevant articles and documents
Chemoselective Perfluoromethylation of Thio- And Selenoamides
Xu, Tao,Xu, Xianhong,Zhang, Jianyu
, (2020)
A chemo- and regioselective perfluoromethylation using thioamides/selenoamides (prepared one step from corresponding lactams) as starting materials has been discovered. The reaction demonstrated complementary chemoselectivity to the C-H trifluoromethylation of (hetero)arenes as well as remarkable functional group compatibility especially toward radical sensitive olefin-, alkyne-, and arylhalide-bearing substrates. The examples of perfluorothio-/selenolated drug molecules indicated application potential of this strategy in drug modification and drug-analogue preparation.
Thio- or seleno-amide compound and preparation method thereof
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Paragraph 0030-0033, (2020/07/24)
The invention discloses a thio- or seleno-amide compound and a preparation method thereof. The preparation method comprises the following steps of dissolving a chlorinated aromatic heterocyclic compound 1 in an EtOH solution, adding 1.0-2.0 times of equivalent thiourea or selenourea, stirring at 50-120 DEG C for 1-8 hours, and reacting to obtain a compound 2, namely the required thio- or seleno-amide compound. Each step of the synthetic route can be amplified, the yield can reach 85 percent, the synthesized compound provides a medical intermediate for synthesizing purine derivatives containingSCF3 or SeCF3, the synthetic route provided by the invention brings a simpler and more effective way for synthesizing compounds with biological activity, the yield is high, large-scale preparation can be realized, and the application prospect is very wide.