871502-87-3Relevant articles and documents
Design, synthesis, and structure–activity relationship study of potent mapk11 inhibitors
Gong, Mengdie,Li, Honglin,Li, Lu,Li, Shiliang,Sun, Hongxia,Tu, Mingyan,Zhao, Zhenjiang,Zhu, Lili
, (2022/01/04)
Huntington’s disease (HD) is a rare single-gene neurodegenerative disease, which can only be treated symptomatically. Currently, there are no approved drugs for HD on the market. Studies have found that MAPK11 can serve as a potential therapeutic target f
Synthesis of 3-Benzylphthalide Derivatives by Using a TDAE Strategy
Ibrahimi, Maroua,Khoumeri, Omar,Abderrahim, Raoudha,Terme, Thierry,Vanelle, Patrice
, p. 283 - 286 (2020/11/23)
A one-pot synthesis of new 3-benzylphthalide derivatives was developed by using a strategy based on tetrakis(dimethylamino)ethylene (TDAE). The reactions in the presence of TDAE of substituted benzyl chlorides with methyl 2-formylbenzoate or of substitute
Indium-Catalyzed C?F Bond Transformation through Oxymetalation/β-Fluorine Elimination to Access Fluorinated Isocoumarins
Yata, Tetsuji,Nishimoto, Yoshihiro,Chiba, Kouji,Yasuda, Makoto
supporting information, p. 8288 - 8294 (2021/05/21)
Fluorinated heterocycles have attracted much attention in the pharmaceutical and agrochemical industries. Many strategies have already been developed to achieve the synthesis of fluorinated heterocycles. Formidable challenges remain, however, in the synthesis of fluorinated isocoumarin derivatives that are among the most alluring structural motifs. Herein, the indium-catalyzed C?F bond transformation of 2-(2,2-difluorovinyl) benzoates is reported, which are readily accessible compounds, to give a diverse array of fluorinated isocoumarins. The present reaction proceeds smoothly using inexpensive reagents: a catalytic amount of indium salt in the presence of zinc salt. A theoretical calculation of potential energy profiles showed that the reaction consists of oxymetalation with the elimination of alkyl halide and the β-fluorine elimination.
Engineering a highly selective probe for ratiometric imaging of H2S: N and revealing its signaling pathway in fatty liver disease
Lai, Huanhua,Li, Wei,Wang, Lu,Yin, Shulu,Yuan, Lin,Zhang, Xiaobing
, p. 7991 - 7999 (2020/08/14)
Hydrogen polysulfides (H2Sn, n > 1) have continuously been proved to act as important signal mediators in many physiological processes. However, the physiological role of H2Sn and their signaling pathways in complex diseases, such as the most common liver
Efficient Heterogeneous CO2 to CO Conversion with a Phosphonic Acid Fabricated Cofacial Iron Porphyrin Dimer
Mohamed, Eman A.,Zahran, Zaki N.,Naruta, Yoshinori
, p. 7140 - 7150 (2017/09/19)
For developing renewable fuels and controlling global warming, catalyst promoted conversion of CO2 to CO is essential. Numerous CO2 to CO conversion molecular catalysts have shown very high activity and stability. For large-scale con
Bioorthogonal double-fluorogenic siliconrhodamine probes for intracellular super-resolution microscopy
Kozma,Estrada Girona,Paci,Lemke,Kele
supporting information, p. 6696 - 6699 (2017/07/10)
A series of double-fluorogenic siliconrhodamine probes were synthesized. These tetrazine-functionalized, membrane-permeable labels allowed site-specific bioorthogonal tagging of genetically manipulated intracellular proteins and subsequent imaging using s
Isomerically Pure Tetramethylrhodamine Voltage Reporters
Deal, Parker E.,Kulkarni, Rishikesh U.,Al-Abdullatif, Sarah H.,Miller, Evan W.
, p. 9085 - 9088 (2016/08/05)
We present the design, synthesis, and application of a new family of fluorescent voltage indicators based on isomerically pure tetramethylrhodamines. These new Rhodamine Voltage Reporters, or RhoVRs, use photoinduced electron transfer (PeT) as a trigger for voltage sensing, display excitation and emission profiles in the green to orange region of the visible spectrum, demonstrate high sensitivity to membrane potential changes (up to 47% ΔF/F per 100 mV), and employ a tertiary amide derived from sarcosine, which aids in membrane localization and simultaneously simplifies the synthetic route to the voltage sensors. The most sensitive of the RhoVR dyes, RhoVR 1, features a methoxy-substituted diethylaniline donor and phenylenevinylene molecular wire at the 5′-position of the rhodamine aryl ring, exhibits the highest voltage sensitivity to date for red-shifted PeT-based voltage sensors, and is compatible with simultaneous imaging alongside green fluorescent protein-based indicators. The discoveries that sarcosine-based tertiary amides in the context of molecular-wire voltage indicators prevent dye internalization and 5′-substituted voltage indicators exhibit improved voltage sensitivity should be broadly applicable to other types of PeT-based voltage-sensitive fluorophores.
Facile construction of pyrrolo[1,2-: B] isoquinolin-10(5 H)-ones via a redox-amination-aromatization-Friedel-Crafts acylation cascade reaction and discovery of novel topoisomerase inhibitors
Wu, Shanchao,Liu, Na,Dong, Guoqiang,Ma, Lin,Wang, Shengzheng,Shi, Wencai,Fang, Kun,Chen, Shuqiang,Li, Jian,Zhang, Wannian,Sheng, Chunquan,Wang, Wei
, p. 9593 - 9596 (2016/08/01)
An efficient redox-amination-aromatization-Friedel-Crafts acylation cascade process from trans-4-hydroxyproline and 2-formylbenzoic acids has been developed for the synthesis of pyrrolo[1,2-b]isoquinolin-10(5H)-ones. Compound 3h was identified as a new potent dual topoisomerase I/II inhibitor.
Asymmetric Organocatalytic Synthesis of 4-Aminoisochromanones via a Direct One-Pot Intramolecular Mannich Reaction
Vetica, Fabrizio,Fronert, Jeanne,Puttreddy, Rakesh,Rissanen, Kari,Enders, Dieter
, p. 4451 - 4458 (2016/12/14)
A highly stereoselective one-pot intramolecular Mannich reaction using 2-oxopropyl-2-formylbenzoates and anilines as substrates, catalyzed by a secondary amine, has been developed. The procedure leads to a new class of 4-aminoisochromanones bearing two ad
An Efficient Entry to syn- and anti-Selective Isoindolinones via an Organocatalytic Direct Mannich/Lactamization Sequence
Bisai, Vishnumaya,Unhale, Rajshekhar A.,Suneja, Arun,Dhanasekaran, Sivasankaran,Singh, Vinod K.
supporting information, p. 2102 - 2105 (2015/05/13)
(Chemical Equation Presented) An organocatalytic direct Mannich-lactamization sequence for the syntheses of pharmacologically important enantioenriched isoindolinones is reported. The method utilizes simple α-amino acids to deliver syn- and anti- selectiv