63635-26-7Relevant academic research and scientific papers
MODIFIED PROTEINS AND PROTEIN DEGRADERS
-
Paragraph 00525; 00528; 00529, (2021/12/08)
Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
Metal-free Synthesis of Spiro-2,2′-benzo[b]furan-3,3′-ones via PhI(OAc)2-Mediated Cascade Spirocyclization
Xing, Qingyu,Liang, Huiyuan,Bao, Mingmai,Li, Xuemin,Zhang, Jingran,Bi, Tianhao,Zhang, Yilin,Xu, Jun,Du, Yunfei,Zhao, Kang
supporting information, p. 4669 - 4673 (2019/09/17)
Treating the benzyl protected 3-hydroxy-1,3-bis(2-hydroxyphenyl)prop-2-en-1-ones solely with PhI(OAc)2 (PIDA) in DCE at room temperature readily furnished the seldom studied spiro-2,2′-benzo[b]furan-3,3′-ones in satisfactory to excellent yields. The hypervalent iodine reagent enables the metal-free cascade spirocyclization resulting in the dual oxidative C?O bond formation. (Figure presented.).
High diastereoselectivity in the yang photocyclization via remote hydrogen abstraction reaction
Jang, Mi,Park, Bong Ser
, p. 1509 - 1514 (2016/10/09)
1-Benzoyl-1-(o-alkoxyphenyl)cyclopropanes undergo Yang photocyclization to form dihydrobenzopyranols in a stereospecific manner. The cyclopropyl group at alpha position to carbonyls gives not only a bias in the most stable geometries of the starting ketones but also conformational restriction on geometries of biradical intermediates. More importantly, intramolecular hydrogen bonds seem to give an additional effect on conformational control of the biradical reactivity.
The ortho-substituent effect on the Ag-Catalysed decarboxylation of benzoic acids
Grainger, Rachel,Cornella, Josep,Blakemore, David C.,Larrosa, Igor,Campanera, Josep M.
, p. 16680 - 16687 (2015/03/05)
A combined experimental and computational investigation on the Ag-catalysed decarboxylation of benzoic acids is reported herein. The present study demonstrates that a substituent at the ortho position exerts dual effects in the decarboxylation event. On one hand, ortho-substituted benzoic acids are inherently destabilised starting materials compared to their meta- And para-substituted counterparts. On the other hand, the presence of an ortho-electron-withdrawing group results in an additional stabilisation of the transition state. The combination of both effects results in an overall reduction of the activation energy barrier associated with the decarboxylation event. Furthermore, the Fujita- Nishioka linear free energy relationship model indicates that steric bulk of the substituent can also exert a negative effect by destabilising the transition state of decarboxylation.
AZOLYLMETHYLENEHYDRAZINE DERIVATIVE AND USE THEREOF
-
Page/Page column 33, (2010/04/25)
An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s), a heteroaryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1
Modulators (inhibitors/ activators) of histone acetyltransferases
-
Page/Page column 5, (2008/06/13)
Disclosed are compounds of the formulae: and method of using the compounds to treat cancer, AIDS, HIV infection, and asthma.
AMIDINOPHENYLPYRUVIC ACID DERIVATIVES
-
, (2008/06/13)
An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.
Cesium fluoride-mediated claisen rearrangements of phenyl propargyl ethers: Substituent effects of an orthoalkoxy group on the benzene ring or modified propargyl residues
Ishikawa, Tsutomu,Mizutani, Akiko,Miwa, Chizue,Oku, Yumie,Komano, Naoko,Takami, Atsuya,Watanabe, Toshiko
, p. 2261 - 2272 (2007/10/03)
The expected 7-alkoxy-2-methylbenzo[b]furans were effectively given in the CsF-mediated Claisen rearrangement of phenyl propargyl ethers with an o-alkoxy substituent on the benzene ring. On the other hand CsF did not affect the production of the corresponding benzo[b]furans when ethers, carrying a propargyl residue modified by either 1,1-dimethyl or 3-ethoxycarbonyl functions, were used as substrates in the rearrangement.
The Steric Effect of Ortho Substituents on the Acidic Hydrolysis of Benzamides
Sotomatsu, Tomoko,Fujita, Toshio
, p. 4443 - 4448 (2007/10/02)
The rate constant, k, for the acidic hydrolysis of a number of substituted benzamides in water and in a dioxane water mixture (1:1 v/v) was measured.The reaction conditions were selected to exclude the electronic effects of substituents on the overall rate as far as possible.The log k value for meta derivatives was almost independent of the electronic effects of substituents.Although the log k value for para derivatives was weakly affected by the through-resonance effect of electron-donating substituents, the value for ortho derivatives was almost linear with the Taft-Kutter-Hansch (TKH) Es steric parameter except for NO2 and Ph.The effective steric effects of these ?-bonded planar substituents were approximated by the averaged value of the two TKH Es constants estimated from the thickness and width of each group.The log k value was also analyzed by using the Charton υ steric parameter.The differences in definition of the υ from the TKH Es parameter seriously distorted the analysis of the ortho substituent effects on the hydrolytic reaction.
