75351-33-6Relevant academic research and scientific papers
Amphiphilic dendrimer, synthesis method thereof, and application of amphiphilic dendrimer as drug delivery system
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Paragraph 0096-0101; 0171-0172; 174-0176, (2021/08/07)
The invention relates to a microenvironment response type amphiphilic dendrimer, a synthesis method thereof, and application of the microenvironment response type amphiphilic dendrimer as a drug delivery system. The microenvironment response type amphiphilic dendrimer is a compound with a structure as shown in a formula (I), a formula (II) or a formula (III) or pharmaceutically acceptable salt of the compound. The compound disclosed by the invention can be used as the nano delivery system based on tumor microenvironment specific response, has good solubility in an aqueous solution, can be self-assembled with a drug in the aqueous solution to form a relatively stable nano compound, can effectively deliver the loaded drug to a tumor site; and can responsively disassembl the nano-drug delivery carrier under corresponding stimulation to achieve the purpose of accurate drug release, so that the drug can be released to the focus part to the greatest extent, and the compound is a novel nano-delivery carrier.
A metal-free reductive N-alkylation of indoles with aldehydes
Clanton, Nicholas A.,Spiller, Taylor E.,Ortiz, Eliezer,Gao, Zhinong,Rodriguez-Poirier, Juan Manuel,Delmonte, Albert J.,Frantz, Doug E.
supporting information, p. 3233 - 3236 (2021/04/05)
A simple metal-free method has been developed for the reductive N-alkylation of indoles employing aldehydes as the alkylating agent and inexpensive Et3SiH as the reductant. A wide range of aromatic and aliphatic aldehydes are viable substrates along with
HETEROBIFUNCTIONAL MOLECULES AS TEAD INHIBITORS
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Paragraph 0275-0276, (2021/09/11)
The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
Chemoselective Cleavage of Si-C(sp3) Bonds in Unactivated Tetraalkylsilanes Using Iodine Tris(trifluoroacetate)
Matsuoka, Keitaro,Komami, Narumi,Kojima, Masahiro,Mita, Tsuyoshi,Suzuki, Kimichi,Maeda, Satoshi,Yoshino, Tatsuhiko,Matsunaga, Shigeki
, p. 103 - 108 (2021/01/13)
Organosilanes are synthetically useful reagents and precursors in organic chemistry. However, the typical inertness of unactivated Si-C(sp3) bonds under conventional reaction conditions has hampered the application of simple tetraalkylsilanes in organic synthesis. Herein we report the chemoselective cleavage of Si-C(sp3) bonds of unactivated tetraalkylsilanes using iodine tris(trifluoroacetate). The reaction proceeds smoothly under mild conditions (-50 °C to room temperature) and tolerates various polar functional groups, thus enabling subsequent Tamao-Fleming oxidation to provide the corresponding alcohols. NMR experiments and density functional theory calculations on the reaction indicate that the transfer of alkyl groups from Si to the I(III) center and the formation of the Si-O bond proceed concertedly to afford an alkyl-λ3-iodane and silyl trifluoroacetate. The developed method enables the use of unactivated tetraalkylsilanes as highly stable synthetic precursors.
Stereoselective, Multicomponent Approach to Quaternary Substituted Hydroindole Scaffolds
Massaro, Nicholas P.,Pierce, Joshua G.
supporting information, p. 5079 - 5084 (2020/07/04)
The Amaryllidaceae alkaloids have been a target of synthesis for decades due to their complex architectures and biological activity. A central feature of these natural product cores is a quaternary substituted hydroindole heterocycle. Building off the fou
One-pot cascade synthesis of azabicycles via the nitro-Mannich reaction and N -alkylation
Disadee, Wannaporn,Ruchirawat, Somsak
supporting information, p. 707 - 711 (2018/02/09)
A one-pot, metal-free process for the synthesis of azabicycles is developed. The key transformations involved a cascade of double intramolecular cyclizations via the nitro-Mannich reaction and N-alkylation, providing various ring systems of azabicycles in
Semisynthesis of Chondroitin Sulfate e Tetrasaccharide from Hyaluronic Acid
Yao, Wang,Zhu, Yong,Zhang, Xiao,Sha, Meng,Meng, Xiangbao,Li, Zhongjun
, p. 14069 - 14077 (2018/11/30)
Chondroitin sulfate (CS) is crucial glycosaminoglycan that regulates key functions of the nervous system. CS-E is one of the key CS subtypes that modulates the biological function of CS. Herein, N-protecting-group-free semisynthesis of CS-E tetrasaccharid
Polymer-Supported Chiral-at-Metal Lewis Acid Catalysts
Larionov, Vladimir A.,Cruchter, Thomas,Mietke, Thomas,Meggers, Eric
supporting information, p. 1457 - 1460 (2017/04/28)
The covalent immobilization of a chiral-at-metal bis-cyclometalated iridium(III) catalyst on a solid support is reported, and its catalytic activity has been investigated. As a catalyst immobilization strategy, a catalyst precursor was tethered to polystyrene macrobeads through an ester or amide linkage and subsequently converted to the immobilized active chiral Lewis acid by treatment with a Br?nsted acid. The amide-linked catalyst displays high robustness and can be recycled multiple times without deterioration of enantioselectivity and only a gradual loss of catalytic activity. Chiral Lewis acid activity was demonstrated as an example for the enantioselective Friedel-Crafts alkylation of indole with an α,β-unsaturated 2-acyl imidazole and for the enantioselective Diels-Alder reactions of an α,β-unsaturated 2-acyl imidazole with 2,3-dihydrofuran or isoprene.
Synthesis and Characterization of Constitutionally Isomeric Oriented Calix[6]arene-Based Rotaxanes
Zanichelli, Valeria,Ragazzon, Giulio,Arduini, Arturo,Credi, Alberto,Franchi, Paola,Orlandini, Guido,Venturi, Margherita,Lucarini, Marco,Secchi, Andrea,Silvi, Serena
, p. 1033 - 1042 (2016/03/01)
Oriented rotaxanes composed of tris(N-phenylureido)calix[6]arene wheel 1 and N,N′-dialkyl viologen-based axles were synthesized in which the span between the diphenylacetyl stoppers at the wheel upper and lower rim and the bis-pyridinium cation portion of
Click reaction based synthesis, antimicrobial, and cytotoxic activities of new 1,2,3-triazoles
Syed Aly, Mohamed Ramadan El,Saad, Hosam Ali,Mohamed, Mosselhi Abdelnabi Mosselhi
, p. 2824 - 2830 (2015/06/08)
Three-motif pharmacophoric models 20a-e and 21-25 were prepared in good yields by CuAAC of two azido substrates 2 and 11 with seven terminal acetylenic derivatives including chalcones 17a-e, theophylline 18 and cholesterol 19. The structure of these compounds was elucidated by NMR, MS, IR spectroscopy and micro analyses. This series was screened as antimicrobial and cytotoxic agents in vitro. Most derivatives showed appreciable antibacterial activity, but they displayed weak cytotoxic, and antifungal activities. Notably, conjugate 25 (cream of the crop) was found to be more active than Ampicillin against Escherichia coli and Staphylococcus aureus and showed appreciable antifungal and cytotoxic activities as well.
