4869-45-8Relevant articles and documents
PYRIDINE DERIVATIVES AS IMMUNOMODULATORS
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Page/Page column 160, (2021/12/31)
Disclosed are pyridine derivatives of formula (I) and a pharmaceutical composition comprising the pyridine derivatives or their pharmaceutically acceptable salts or stereoisomers thereof, and at least one pharmaceutically acceptable carrier or excipient, which are useful as key intermediate for the synthesis of compounds to inhibit PD-1/PD-L1 signaling pathway or capable of inhibiting PD-1/PD-L1 signaling pathway.
C-H trifluoromethylations of 1,3-dimethyluracil and reactivity of the products in C-H arylations
Cernova, Miroslava,Pohl, Radek,Klepetarova, Blanka,Hocek, Michal
, p. 1159 - 1171 (2014/05/20)
Diverse electrophilic, nucleophilic and radical C-H trifluoromethylations of 1,3-dimethyluracil were systematically studied in order to prepare either 5- or 6-(trifluoromethyl)uracil derivatives. Electrophilic reagents led only to dimeric bis-uracil products, whereas the radical trifluoromethylation by CF 3SO2Na in presence of t-BuOOH gave 1,3-dimethyl-5- (trifluoromethyl)uracil (2) in good yield. The 6-(trifluoromethyl)uracil derivative 3 was only prepared in low yield and in a mixture with 2 by Ir-catalyzed borylation followed by treatment with the Togni's reagent. Attempted Pd-catalyzed C-H arylations of 2 in the presence of Cs 2CO3 gave mixtures of de-trifluoromethylated products, whereas the reaction with 4-iodotoluene in the presence of CsF gave the desired 6-aryl-5-trifluoromethyluracil derivative 8 in moderate yield and the reaction was not general for other aryl halides.
Oxidation of 1,3-Dimethylthymine with Cumene Hydroperoxide catalysed by 5,10,15,20-tetraarylporphyrinatomanganese(III) Chlorides
Gulati, Anju,Chauhan, S. M. S.
, p. 42 - 42 (2007/10/03)
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