- NOVEL TRF1 MODULATORS AND ANALOGUES THEREOF
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Novel TRF1 modulators and analogues thereof. There is provided compounds of Formula I, wherein R, R1, R2 and X have meanings written in the description. Such compounds are useful as TRF1 inhibitors and, for that reason, as medicaments, in the treatment of cancer, particularly high cancer stem cell cancer like glioblastoma and lung cancer, and can be also useful for the development of additional TRF1 inhibitors and increasing knowledge about TRF1 activity.
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Paragraph 0047; 0064-0065; 0112-0113
(2020/03/26)
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- Palladium-Catalyzed Site-Selective Fluorination of Unactivated C(sp3)-H Bonds
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The transition-metal-catalyzed direct C-H bond fluorination is an attractive synthetic tool toward the preparation of organofluorines. While many methods exist for the direct sp3 C-H functionalization, site-selective fluorination of unactivated sp3 carbons remains a challenge. Direct, highly site-selective and diastereoselective fluorination of aliphatic amides via a palladium-catalyzed bidentate ligand-directed C-H bond functionalization process on unactivated sp3 carbons is reported. With this approach, a wide variety of β-fluorinated amino acid derivatives and aliphatic amides, important motifs in medicinal and agricultural chemistry, were prepared with palladium acetate as the catalyst and Selectfluor as the fluorine source.
- Miao, Jinmin,Yang, Ke,Kurek, Martin,Ge, Haibo
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supporting information
p. 3738 - 3741
(2015/08/18)
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- Neighbouring group effects promote substitution reactions over elimination and provide a stereocontrolled route to chloramphenicol
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In reactions of β-brominated valine and p-nitrophenylalanine derivatives to give β-hydroxy amino acid derivatives the carboxyl group, when protected as an amide, exerts a neighbouring group effect to facilitate the substitution process, and reduce competing elimination reactions. As a consequence of the effect, the (2R,3R)- and (2R,3S)-stereoisomers of 3-bromo-N-tert-butyl-N(α)-phthaloyl-p-nitrophenylalaninamide both react to give (2S,3R)-3-hydroxy-N-tert-butyl-N(α)-phthaloyl-p-nitrophenylalaninamid e, providing a stereoconvergent route to chloramphenicol.
- Easton, Christopher J.,Hutton, Craig A.,Merrett, Martin C.,Tiekink, Edward R. T.
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p. 7025 - 7036
(2007/10/03)
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