7107-59-7Relevant academic research and scientific papers
Positioning of an unprecedented 1,5-oxaza spiroquinone scaffold into SMYD2 inhibitors in epigenetic space
Dhorma, Lama Prema,Kim, Mi-hyun,Maeng, Han-Joo,Maturi, Arunkranthi,Mirzaei, Anvar,Nangunuri, Bhargav Gupta,Ragam, Rao,Teli, Mahesh K.,Venkanna, Arramshetti,Vo, Dang-Khoa
supporting information, (2021/10/16)
Lysine methyltransferases are important regulators of epigenetic signaling and are emerging as a novel drug target for drug discovery. This work demonstrates the positioning of novel 1,5-oxaza spiroquinone scaffold into selective SET and MYND domain-conta
PIFA-Promoted, Solvent-Controlled Selective Functionalization of C(sp2)-H or C(sp3)-H: Nitration via C-N Bond Cleavage of CH3NO2, Cyanation, or Oxygenation in Water
Mudithanapelli, Chandrashekar,Dhorma, Lama Prema,Kim, Mi-Hyun
supporting information, (2019/05/07)
A novel nitration (via C(sp3)-N breaking/C(sp2)-N formation with CH3NO2) mediated by [bis(trifluoroacetoxy)iodo]benzene (PIFA) is described. The NO2 transfer from CH3NO2 to the aromatic group of the substrate is possible with careful selection of the solvent, NaX, and oxidant. In addition, the solvent-controlled C(sp2)-H functionalization can shift to an α-C(sp3)-H functionalization (cyanation or oxygenation) of the α-C(sp3)-H of cyclic amines.
One stone two birds: Cobalt-catalyzed in situ generation of isocyanates and benzyl alcohols for the synthesis of N-aryl carbamates
Li, Sida,Khan, Ruhima,Zhang, Xia,Yang, Yong,Wang, Zheting,Zhan, Yong,Dai, Yuze,Liu, Yue-E,Fan, Baomin
, p. 5891 - 5896 (2019/06/24)
An efficient method for the synthesis of N-aryl carbamates from N-Boc-protected amines has been developed. The cobalt-catalyzed in situ generation of isocyanates from N-Boc-protected amines and benzyl alcohols from benzyl formates has been achieved for the first time, which in turn furnished the corresponding benzyl carbamates in moderate to high yields. The reaction was catalyzed by CoI2 with tris-(4-dimethylaminophenyl)-phosphine as the ligand and zinc powder as the reductant. The developed reaction conditions were found to be compatible for aromatic amines with both electron-donating and -withdrawing substituents.
NOVEL SPIROQUINONE DERIVATIVE COMPOUND, PRODUCTION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING NEUROLOGICAL DISORDERS WHICH CONTAINS SAME AS ACTIVE INGREDIENT
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Paragraph 0148; 0149, (2018/11/21)
The present invention relates to a novel spiroquinone derivative compound, a production method thereof, and a pharmaceutical composition for preventing or treating neurological disorders which contains the compound as an active ingredient, and it has been
Bazedoxifene-scaffold-based mimetics of solomonsterols A and B as novel pregnane x receptor antagonists
Hodnik, ?iga,Peterlin Ma?i?, Lucija,Toma?i?, Tihomir,Smodi?, Domen,D'Amore, Claudio,Fiorucci, Stefano,Kikelj, Danijel
, p. 4819 - 4833 (2014/07/07)
Pregnane X receptor (PXR), a member of the NR1I nuclear receptor family, acts as a xenobiotic sensor and a paramount transcriptional regulator of drug-metabolizing enzymes and transporters. The overexpression of PXR in various cancer cells indicates the importance of PXR as a drug target for countering multidrug resistance in anticancer treatments. We describe the discovery of novel bazedoxifene-scaffold-based PXR antagonists inspired by the marine sulfated steroids solomonsterol A and B as natural leads. A luciferase reporter assay on a PXR-transfected HepG2 cell line identified compounds 19-24 as promising PXR antagonists. Further structure-activity relationship studies of the most active PXR antagonist from the series (compound 20, IC50 = 11 μM) revealed the importance of hydroxyl groups as hydrogen-bond donors for PXR antagonistic activity. PXR antagonists 20 and 24 (IC50 = 14 μM), in addition to the downregulation of PXR expression, exhibited inhibition of PXR-induced CYP3A4 expression, which illustrates their potential to suppress PXR-regulated phase-I drug metabolism.
One-pot catalysis of dehydrogenation of cyclohexanones to phenols and oxidative Heck coupling: Expedient synthesis of coumarins
Kim, Donghee,Min, Minsik,Hong, Sungwoo
supporting information, p. 4021 - 4023 (2013/07/26)
One-pot reactions leading to highly functionalized coumarins have been developed via a Pd(ii)-catalyzed dehydrogenation-oxidative Heck-cyclization process.
A facile protocol for N-Cbz protection of amines in PEG-600
Zhang, Chun Lin,Zhang, Dong Feng,Zhao, Hong Yi,Lin, Zi Yun,Huang, Hai Hong
experimental part, p. 789 - 792 (2012/08/08)
An efficient and eco-friendly protocol for the chemoselective N-benzyloxycarbonylation of amines was described. The reaction of amines with benzyl chloroformate (Cbz-Cl) in the presence of PEG-600 at room temperature afforded the corresponding N-Cbz derivatives in excellent yields. The method is applicable to the N-Cbz protection of aliphatic (acyclic and cyclic) and aromatic amines.
Synthesis of a β-cyclodextrin derivate and its molecular recognition behavior on modified glassy carbon electrode by diazotization
Wang, Xiuhua,Fan, Hao,Zhang, Fan,Qi, Yantao,Qiu, Wenwei,Yang, Fan,Tang, Jie,He, Pingang
experimental part, p. 7815 - 7820 (2010/11/17)
A novel β-cyclodextrin (β-CD) derivative containing mono-phenylamino (MPA-β-CD) was newly synthesized by classical Mitsunobu reaction in good yield, and its structure has been confirmed by 1H NMR, 13C NMR and electrospray ionization
A mild and efficient chemoselective: N-benzyloxycarbonylation of amines using TBAB a catalyst under solvent-free conditions
Babu, Kothamasu Suresh,Rao, Vidadala Rama Subba,Rao, Ravu Ranga,Babu, Sakhamuri Sivaram,Rao, Janaswami Madhusudana
experimental part, p. 393 - 396 (2009/10/17)
We describe a mild and efficient method for the chemoselective N-benzyloxycarbonylation of amines by treatment amines and aminoesters with benzyloxycarbonyl chloride (Cbz-Cl) in the presence of TBAB under solvent-free in excellent yields. The method is ge
FUSED HETEROCYCLIC DERIVATIVES AND USE THEREOF
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Page/Page column 130-131, (2010/01/29)
The present invention provides a fused heterocyclic derivative having a strong kinase inhibitory activity and use thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specificatio
