62135-86-8Relevant academic research and scientific papers
Non-metal Lewis acid-catalyzed cross-Claisen condensation for β-keto esters
Han, Zhengyu,Huang, Hai,Meng, Fuliang,Yang, Zhenkun,Zhang, Tianyu,Zhou, Dapeng
supporting information, p. 9163 - 9166 (2021/11/16)
In this work, we disclose a new catalytic and highly chemoselective cross-Claisen condensation of esters. In the presence of TBSNTf2 as a non-metal Lewis acid, various esters can undergo cross-Claisen condensation to form β-keto esters which are important building blocks. Compared with the traditional Claisen condensation, this process, employing silyl ketene acetals (SKAs) as carbonic nucleophiles to achieve cross-Claisen condensation, requires mild conditions and has good tolerance of functional groups. This journal is
Novel quinoline derivative inhibitor
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Paragraph 1070; 1078-1080, (2020/03/12)
The invention provides a novel quinoline derivative inhibitor, which has a structure represented by the following general formula (I). According to the invention, the compound provided by the invention can selectively inhibit tyrosine kinase TAM family/an
TAM family kinase and/or CSF1R kinase inhibitor and application thereof
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, (2019/08/06)
The invention provides a novel inhibitor compound shown in a general formula (I). The compound has good kinase inhibition activity and can be used for preventing and/or treating diseases mediated by abnormal expression of TAM family kinase and/or a ligand thereof. The compound can target CSF1R kinase and can be used for preventing and/or treating diseases mediated by abnormal expression of a TAM family kinase receptor and/or a CSF1R kinase receptor and/or ligands thereof.
PYRIDONE DERIVATIVE HAVING TETRAHYDROPYRANYLMETHYL GROUP
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Paragraph 0360-0363, (2017/07/14)
The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl. The present disclosure provides pyridone derivatives having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or salts thereof, or crystals of the compounds or the salts, wherein R1, R2, R3, R4, R5, W, X, Y, and Z are each as defined in the specification:
Synthesis of aryl β-ketoesters by opening of aryl epoxides with ethyl diazoacetate catalyzed by BF3OEt2
Rao, D. Chandra,Reddy, D. Kumar,Shekhar,Chinababu,Rao, Ch. Bhujanga,Venkateswarlu
, p. 356 - 358 (2014/05/06)
A facile synthesis of 4-aryl substituted β-ketoesters from the reaction aryl epoxides with ethyl diazoacetate, in presence of BF 3OEt2 has been described with excellent yields.
Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor
Wang, Hsiao-Chun,Jagtap, Ajit Dhananjay,Chang, Pei-Teh,Liu, Jia-Rong,Liu, Chih-Peng,Tseng, Hsiang-Wen,Chen, Grace Shiahuy,Chern, Ji-Wang
, p. 312 - 334 (2014/08/05)
Bioisosteric replacement of acylureido moiety in 6-acylureido-3- pyrrolylmethylidene-2-oxoindoline derivatives resulted in a series of malonamido derivatives with indolin-2-one scaffold (11-14). Further conformational restrictions of the malonamido moiety led to 2-oxo-1,2-dihydropyridine (21-25) or a 4-oxo-1,4-dihydropyridine derivatives (31-36). 4-Oxo-1,4-dihydropyridine derivatives were more potent Aurora B inhibitors than their 2-oxo-1,2- dihydropyridine counterparts and demonstrated cytotoxicities against A549 and HepG2 cells in the submicromolar range. In A549 cells, 31h decreased phosphorylation of histone H3, triggered polyploidy, induced expression of pro-apoptotic Fas and FasL with subsequent activation of caspase 8, resulting into apoptosis. In a Huh7-xenograft mouse model, 31h demonstrated potent in vivo efficacy with a daily dose of 5 mg/kg.
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains
Li, Amin,Ouyang, Yabo,Wang, Ziyun,Cao, Yuanyuan,Liu, Xiangyi,Ran, Li,Li, Chao,Li, Li,Zhang, Liang,Qiao, Kang,Xu, Weisi,Huang, Yang,Zhang, Zhili,Tian, Chao,Liu, Zhenming,Jiang, Shibo,Shao, Yiming,Du, Yansheng,Ma, Liying,Wang, Xiaowei,Liu, Junyi
, p. 3593 - 3608 (2013/06/27)
Novel 6-substituted-4-cycloalkyloxy-pyridin-2(1H)-ones were synthesized as non-nucleoside reverse transcriptase inhibitors (NNRTIs), and their biological activity was evaluated. Most of the compounds, especially 26 and 22, bearing a 3-isopropyl and 3-iodine group, respectively, exhibited highly potent activity against wild-type HIV-1 strains and those resistant to reverse transcriptase inhibitors (RTIs). The diastereoisomers of 26-trans and 26-cis were synthesized separately and confirmed with HPLC and NOESY spectra. The 26-trans isomers had an activity about 400-fold more potent than that of 26-cis. The pair of 26-trans enantiomers, one of the most potent inhibitors with EC50 of 4 nM and selectivity index (SI) of 75000, was highly effective against a panel of RTIs-resistant strains with single (Y181C and K103N) or double (A17) mutations in reverse transcriptase. The results suggest that these novel pyridinone derivatives have the potential to be further developed as new antiretroviral drugs with improved antiviral efficacy and drug resistance profile.
Modulation of luminescence intensity of lanthanide complexes by photoinduced electron transfer and its application to a long-lived protease probe
Terai, Takuya,Kikuchi, Kazuya,Iwasawa, Shin-Ya,Kawabe, Takao,Hirata, Yasunobu,Urano, Yasuteru,Nagano, Tetsuo
, p. 6938 - 6946 (2007/10/03)
Luminescent lanthanide complexes (Tb3+, Eu3+, etc.) have excellent properties for biological applications, including extraordinarily long lifetimes and large Stokes shifts. However, there have been few reports of lanthanide-based functional probes, because of the difficulty in designing suitable complexes with a luminescent on/off switch. Here, we have synthesized a series of complexes which consist of three moieties: a lanthanide chelate, an antenna, and a luminescence off/on switch. The antenna is an aromatic ring which absorbs light and transmits its energy to the metal, and the switch is a benzene derivative with a different HOMO level. If the HOMO level is higher than a certain threshold, the complex emits no luminescence at all, which indicates that the lanthanide luminescence can be modulated by photoinduced electron transfer (PeT) from the switch to the sensitizer. This approach to control lanthanide luminescence makes possible the rational design of functional lanthanide complexes, in which the luminescence property is altered by a biological reaction. To exemplify the utility of our approach to the design of lanthanide complexes with a switch, we have developed a novel protease probe, which undergoes a significant change in luminescence intensity upon enzymatic cleavage of the substrate peptide. This probe, combined with time-resolved measurements, was confirmed in model experiments to be useful for the screening of inhibitors, as well as for clinical diagnosis.
