3896-29-5Relevant articles and documents
Preparation method of 2, 4-difluoro-3-nitrobenzoic acid
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Paragraph 0113-0115; 0129; 0134; 0135-0139, (2020/07/12)
The invention discloses a preparation method of 2, 4-difluoro-3-nitrobenzoic acid. The preparation method comprises the following technical key points of: carrying out amino protection on 2, 6-difluoroaniline to obtain a compound V; reacting the compound
Regioselective, nucleophilic activation of C&F bonds in o-fluoroanilines
Hough, Sarita E.,Hargrove, Willie R.,Deck, Paul A.
, p. 121 - 126 (2019/07/09)
Reactions of ortho-fluorinated anilines with stoichiometric Ti(NMe2)4 in mesitylene (typically for 23 h at 120 °C) afforded moderate to high yields of the corresponding N,N-dimethyl-1,2-phenylenediamine derivatives resulting from def
Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling
Liu, Longbin,Lee, Matthew R.,Kim, Joseph L.,Whittington, Douglas A.,Bregman, Howard,Hua, Zihao,Lewis, Richard T.,Martin, Matthew W.,Nishimura, Nobuko,Potashman, Michele,Yang, Kevin,Yi, Shuyan,Vaida, Karina R.,Epstein, Linda F.,Babij, Carol,Fernando, Manory,Carnahan, Josette,Norman, Mark H.
, p. 2215 - 2234 (2016/04/26)
One of the challenges for targeting B-RafV600E with small molecule inhibitors had been achieving adequate selectivity over the wild-type protein B-RafWT, as inhibition of the latter has been associated with hyperplasia in normal tissues. Recent studies suggest that B-Raf inhibitors inducing the 'DFG-in/αC-helix-out' conformation (Type IIB) likely will exhibit improved selectivity for B-RafV600E. To explore this hypothesis, we transformed Type IIA inhibitor (1) into a series of Type IIB inhibitors (sulfonamides and sulfamides 4-6) and examined the SAR. Three selectivity indices were introduced to facilitate the analyses: the B-RafV600E/B-RafWT biochemical (bS), cellular (cS) selectivity, and the phospho-ERK activation (pA). Our data indicates that α-branched sulfonamides and sulfamides show higher selectivities than the linear derivatives. We rationalized this finding based on analysis of structural information from the literature and provided evidence for a monomeric B-Raf-inhibitor complex previously hypothesized to be responsible for the desired B-RafV600E selectivity.