77826-30-3Relevant academic research and scientific papers
EP300/CREBBP INHIBITOR
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Paragraph 0355; 0356; 0391; 0392, (2020/05/30)
The present invention provides a compound having excellent histone acetyltransferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.
Enantioselective Copper Catalyzed Alkyne-Azide Cycloaddition by Dynamic Kinetic Resolution
Liu, En-Chih,Topczewski, Joseph J.
supporting information, p. 5135 - 5138 (2019/03/29)
The copper(I) catalyzed alkyne-azide cycloaddition (CuAAC), a click reaction, is one of the most powerful catalytic reactions developed during the last two decades. Conducting CuAAC enantioselectively would add a third dimension to this reaction and would
Lewis Acid Catalyzed Transfer Hydromethallylation for the Construction of Quaternary Carbon Centers
Walker, Johannes C. L.,Oestreich, Martin
supporting information, p. 15386 - 15389 (2019/10/28)
The design and gram-scale synthesis of a cyclohexa-1,4-diene-based surrogate of isobutene gas is reported. Using the highly electron-deficient Lewis acid B(C6F5)3, application of this surrogate in the hydromethallylation of electron-rich styrene derivatives provided sterically congested quaternary carbon centers. The reaction proceeds by C(sp3)?C(sp3) bond formation at a tertiary carbenium ion that is generated by alkene protonation. The possibility of two concurrent mechanisms is proposed on the basis of mechanistic experiments using a deuterated surrogate.
Visible-Light-Mediated Ring-Opening Strategy for the Regiospecific Allylation/Formylation of Cycloalkanols
Wang, Junlei,Huang, Binbin,Shi, Chengcheng,Yang, Chao,Xia, Wujiong
, p. 9696 - 9706 (2018/09/06)
Here we describe a straightforward and efficient approach for regiospecific introduction of an allyl group into cycloalkanol molecules employing a visible-light-mediated ring-opening strategy. A wide range of distally allylated or formylated ketones is fu
Catalytic Ring-Opening of Cyclic Alcohols Enabled by PCET Activation of Strong O-H Bonds
Yayla, Hatice G.,Wang, Huaiju,Tarantino, Kyle T.,Orbe, Hudson S.,Knowles, Robert R.
supporting information, p. 10794 - 10797 (2016/09/09)
We report a new photocatalytic protocol for the redox-neutral isomerization of cyclic alcohols to linear ketones via C-C bond scission. Mechanistic studies demonstrate that key alkoxy radical intermediates in this reaction are generated via the direct homolytic activation of alcohol O-H bonds in an unusual intramolecular PCET process, wherein the electron travels to a proximal radical cation in concert with proton transfer to a weak Br?nsted base. Effective bond strength considerations are shown to accurately forecast the feasibility of alkoxy radical generation with a given oxidant/base pair.
Auto de-bromine-coupling reactions of 1-aryl-7-bromocycloheptenes
Lee, Gon-Ann,Lee, Hsin-Yi,Wang, Wen-Chieh,Cherng, Chih-Hwa
, p. 2956 - 2961 (2014/04/17)
Auto de-bromine-coupling reactions of 1-aryl-7-bromocycloheptenes to a new series of [7-6-6] tricyclic system were described. A variety of substituents at the para-position of the phenyl were amenable to this transformation, including electron-donating groups and halides. The presence of electron-donating groups resulted in a more efficient reaction, with higher yields than the case of halides.
