14/10/2022 - Page 9 of 9 - Indole Building Blocks

Duan, Shengguo’s team published research in Advanced Synthesis & Catalysis in 2020-05-03 | 4771-48-6

Advanced Synthesis & Catalysis published new progress about [4+2] Cycloaddition reaction (stereoselective). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Application of C10H9NO.

Duan, Shengguo; An, Yuehui; Xue, Bing; Chen, Yidian; Zhang, Wan; Xu, Ze-Feng; Li, Chuan-Ying published the artcile< Synthesis of Pyrido[2,3-b]indole Derivatives via Rhodium-Catalyzed Cyclization of Indoles and 1-Sulfonyl-1,2,3-triazoles>, Application of C10H9NO, the main research area is indole sulfonyltriazole preparation rhodium catalyst diastereoselective cycloaddition; pyridoindole preparation.

Acyloxy-substituted α,β-unsaturated imines generated in-situ from triazoles acts as aza-[4C] synthons and be trapped by indoles in a stepwise [4 + 2] cycloaddition reaction, thus providing rapid access to valuable pyrido[2,3-b]indoles in high yields. Attractive features of this reaction system included operational simplicity, readily available substrates, construction of sterically demanding quaternary centers and convenient derivatization using triflate.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Tian, Minggang’s team published research in Chemical Communications (Cambridge, United Kingdom) in 2019 | 950846-89-6

Chemical Communications (Cambridge, United Kingdom) published new progress about Autophagy. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Synthetic Route of 950846-89-6.

Tian, Minggang; Liu, Chuang; Dong, Baoli; Zuo, Yujing; Lin, Weiying published the artcile< A dual-site controlled ratiometric probe revealing the simultaneous down-regulation of pH in lysosomes and cytoplasm during autophagy>, Synthetic Route of 950846-89-6, the main research area is ratiometric fluorescent probe lysosome cytoplasm autophagy hydrogen ion.

In this work, a unique dual-site controlled fluorescent probe was presented for the sensitive and concurrent detection of pH in the cytoplasm and lysosomes. With the probe, the simultaneous down-regulation of pH in the lysosomes and cytoplasm during autophagy has been successfully revealed for the first time.

Wang, Lei’s team published research in Nucleic Acids Research in 2018-09-28 | 101083-92-5

Nucleic Acids Research published new progress about Aminopyridines Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 101083-92-5 belongs to class indole-building-block, and the molecular formula is C7H5N3O2, HPLC of Formula: 101083-92-5.

Wang, Lei; Taniguchi, Yosuke; Okamura, Hidenori; Sasaki, Shigeki published the artcile< Modification of the aminopyridine unit of 2'-deoxyaminopyridinyl-pseudocytidine allowing triplex formation at CG interruptions in homopurine sequences>, HPLC of Formula: 101083-92-5, the main research area is aminopyridine derive sequence synthesis CG inversion site.

The antigene strategy based on site-specific recognition of duplex DNA by triplex DNA formation has been exploited in a wide range of biol. activities. However, specific triplex formation is mostly restricted to homo-purine strands within the target duplex DNA, due to the destabilizing effect of CG and TA inversion sites where there is an absence of natural nucleotides that can recognize the CG and TA base pairs. Hence, the design of artificial nucleosides, which can selectively recognize these inversion sites with high affinity, should be of great significance. Recently, we determined that 2-amino-3-methylpyridinyl pseudo-dC (3MeAP-VdC) possessed significant affinity and selectivity toward a CG inversion site and showed effective inhibition of gene expression. We now describe the design and synthesis of new modified aminopyridine derivatives by focusing on small chem. modification of the aminopyridine unit to tune and enhance the selectivity and affinity toward CG inversion sites. Remarkably, we have newly found that 2-amino-4-methoxypyridinyl pseudo-dC (4OMeAP-VdC) could selectively recognize the CG base pair in all four adjacent base pairs and form a stable triplex structure against the promoter sequence of the human gene including multiple CG inversion sites.

Ermoli, Antonella’s team published research in Journal of Medicinal Chemistry in 2009-07-23 | 101083-92-5

Journal of Medicinal Chemistry published new progress about Molecular modeling. 101083-92-5 belongs to class indole-building-block, and the molecular formula is C7H5N3O2, Product Details of C7H5N3O2.

Ermoli, Antonella; Bargiotti, Alberto; Brasca, Maria Gabriella; Ciavolella, Antonella; Colombo, Nicoletta; Fachin, Gabriele; Isacchi, Antonella; Menichincheri, Maria; Molinari, Antonio; Montagnoli, Alessia; Pillan, Antonio; Rainoldi, Sonia; Sirtori, Federico Riccardi; Sola, Francesco; Thieffine, Sandrine; Tibolla, Marcellino; Valsasina, Barbara; Volpi, Daniele; Santocanale, Corrado; Vanotti, Ermes published the artcile< Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure-Activity Relationships>, Product Details of C7H5N3O2, the main research area is cell division cycle 7 kinase inhibitor pyrrolopyridine preparation SAR.

Cdc7 kinase has recently emerged as an attractive target for cancer therapy and low-mol.-weight inhibitors of Cdc7 kinase have been found to be effective in the inhibition of tumor growth in animal models. In this paper, we describe synthesis and structure-activity relationships of new 1H-pyrrolo[2,3-b]pyridine derivatives identified as inhibitors of Cdc7 kinase. Progress from (Z)-2-phenyl-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-3,5-dihydro-4H-imidazol-4-one to [(Z)-2-(benzylamino)-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-1,3-thiazol-4(5H)-one] (I), a potent ATP mimetic inhibitor of Cdc7 kinase with IC50 value of 7 nM, is also reported.

Journal of Medicinal Chemistry published new progress about Molecular modeling. 101083-92-5 belongs to class indole-building-block, and the molecular formula is C7H5N3O2, Product Details of C7H5N3O2.

Luo, Wenfeng’s team published research in Analytical Methods in 2019 | 950846-89-6

Analytical Methods published new progress about Fluorescent indicators. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Quality Control of 950846-89-6.

Luo, Wenfeng; Lei, Mengmeng; Wang, Yuan; Gao, Haolei; Wang, Yang; Zhou, Qihang; Xu, Zhihong; Yang, Fengling published the artcile< An indole-rhodamine-based ratiometric fluorescent probe for Pd2+ determination and cell imaging>, Quality Control of 950846-89-6, the main research area is indole rhodamine fluorescent probe lead cell imaging.

A ratiometric fluorescent probe for Pd2+ has been constructed through appending indole to rhodamine B. The response process of Pd2+ to probe was also verified by UV-vis, fluorescence, ESI-MS, 1H NMR and d. functional theory calculation Moreover, the highly sensitive and selective probe was successfully applied to monitor Pd2+ in living cells.

Analytical Methods published new progress about Fluorescent indicators. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Quality Control of 950846-89-6.

Liu, Boya’s team published research in ACS Applied Polymer Materials in 2022-09-09 | 399-76-8

ACS Applied Polymer Materials published new progress about Crosslinking. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Safety of 5-Fluoroindole-2-carboxylic acid.

Liu, Boya; Liu, Yang; Liu, Xiangyang published the artcile< Enhanced Thermal Conductivity of All-Organic Aramid Nanofiber Films via Interfacial Coupling Reaction>, Safety of 5-Fluoroindole-2-carboxylic acid, the main research area is thermal conductivity organic aramid nanofiber film interfacial coupling.

It is still a great challenge to prepare intrinsically all-organic thermal conductive membrane with high in-plane and through-plane thermal conductivity Herein, we designed an all-organic aramid nanofiber thin film with in-plane and through-plane thermal conductivity as high as 15.7 and 0.26 W/mK, resp., through one step fluorination utilizing F2/N2. We proved that direct fluorination could induce the coupling reaction of benzene rings in neighboring aramid macromols. to form numerous covalent crosslinking bonds among aramid nanofibers. Benefiting from the crosslinking behavior, interfacial thermal resistance between the nanofibers was suppressed to some extent, thereby leading to enhancement of in-plane and through-plane thermal conductivity by 78.8% and 271.7%, resp., compared with the unmodified membranes. In addition, the thin films also possess high mech. strength and elec. insulation, which promote its application potential in flexible electronic fields.

Zi, Weiwei’s team published research in Journal of the American Chemical Society in 2015-03-11 | 4771-48-6

Journal of the American Chemical Society published new progress about Acetals Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (indolyl, propargyl). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Category: indole-building-block.

Zi, Weiwei; Wu, Hongmiao; Toste, F. Dean published the artcile< Gold(I)-Catalyzed Dearomative Rautenstrauch Rearrangement: Enantioselective Access to Cyclopenta[b]indoles>, Category: indole-building-block, the main research area is cyclopentaindole cyclopentapyrrole enantioselective diastereoselective preparation; stereoselective Rautenstrauch rearrangement indolylpropynyl pyrrolylpropynyl acetal Segphos digold complex; dearom diastereoselective enantioselective Rautenstrauch rearrangement indolylpropynyl pyrrolylpropynyl acetal; methylcyclopentaindolecarboxylate mol crystal structure.

In the presence of a DTBM-Segphos digold complex and AgSbF6, indolylpropynyl acetals I (R = H, 5-F, 5-Br, 5-Me, 5-MeO, 4-Me, 6-MeO, 6-Cl, 7-Me; R1 = Me, Et, Bu; R3 = MeO2C, EtO2C, H2C:CHCH2O2C, EtCO, PhCO; Ts = 4-MeC6H4SO2) and a pyrrolylpropynyl acetal underwent enantioselective dearomative Rautenstrauch rearrangements to yield (after hydrolysis) nonracemic cyclopenta[b]indoles II (R = H, 5-F, 5-Br, 5-Me, 5-MeO, 4-Me, 6-MeO, 6-Cl, 7-Me; R1 = Me, Et, Bu; R3 = MeO2C, EtO2C, H2C:CHCH2O2C, EtCO, PhCO) and a cyclopentapyrrolecarboxylate in 46-91% yields and in 71-98% ee. The structures of II (R = 4-Me; R1 = Me; R2 = MeO2C) and of a reduction product derived from II (R = H; R1 = Me; R2 = MeO2C) were determined by X-ray crystallog.