165114-87-4Relevant articles and documents
UREA DERIVATIVE AND USE THEREFOR
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Paragraph 0204; 0240, (2018/07/29)
The purpose of the present invention is to provide a compound with inhibitory activity on Discoidin Domain Receptor 1. The present invention provides a urea derivative represented by the formula below or a pharmaceutically acceptable salt thereof.
New 4-pentafluorosulfanyl and 4-perfluoroalkylthio derivatives of 1-chloro-2-nitro- and 1-chloro-2,6-dinitrobenzenes
Sipyagin, Alexey M.,Enshov, Vyacheslav S.,Kashtanov, Sergei A.,Bateman, Colin P.,Mullen, Brian D.,Tan, Ying-Teck,Thrasher, Joseph S.
, p. 1305 - 1316 (2007/10/03)
New 4-pentafluorosulfanyl and 4-perfluoroalkylthio derivatives of 1-chloro-2-nitrobenzene and 1-chloro-2,6-dinitrobenzene were prepared from the corresponding bis(4-chloro-3-nitrophenyl)disulfide and bis(4-chloro-3,5-dinitrophenyl)disulfide, respectively. The SF5 derivatives were obtained by fluorination of the disulfides with AgF2 according to Sheppard's method, while perfluoroalkylation was carried out by means of thermolytic reactions with xenon(II) bis(perfluoroalkylcarboxylates). The introduction of fluorine-containing, electron-withdrawing substituents into the aromatic ring (in the presence of other deactivating groups) reinforces the activation of the halogen substituent towards nucleophilic attack. Several nucleophilic substitution reactions have been carried out with these compounds, and as a result, some N- and S-containing groups were introduced in the benzene ring. For example, the previously unknown SF5, CF3S, and C2F5S analogues of trifluralin (Treflan) were prepared and characterized. Additional synthetic possibilities for heterocyclic chemistry are presented on the basis of reactions of the new 1-chloro-2,6-dinitrobenzene derivatives with ethyl thioglycolate wherein fluorine-containing derivatives of benzothiazole N-oxide were obtained as the main products.
