Tag: 300-400

Imberdis, Thibaut; Fanning, Saranna; Newman, Andrew; Ramalingam, Nagendran; Dettmer, Ulf published an article in 2019, the title of the article was Studying α-synuclein conformation by intact-cell cross-linking.Application of 79642-50-5 And the article contains the following content:

β-Sheet-rich aggregates of α-synuclein (αS) are the hallmark neuropathol. of Parkinson’s disease (PD) and related synucleinopathies, whereas the native conformations of αS in healthy cells are under debate. Crosslinking analyses in intact cells detect a large portion of endogenous αS in apparent multimeric states, most notably as putative tetramers (αS60) that run around 60 kDa on SDS-PAGE, but also point at the dynamic nature of cellular αS states. Standardization of αS crosslinking methods will facilitate efforts to study the effects of genetic, pharmacol., and environmental factors on αS conformation. Here, we present detailed protocols for crosslinking cellular αS multimers in cultured cells and brain tissues. These protocols will benefit future studies aimed at characterizing αS conformation in its cellular environment, both at steady state and upon perturbation, be it chronic or acute. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Application of 79642-50-5

The Article related to parkinson disease alpha synuclein cell brain, chemical cross-linking, multimer, parkinson’s disease, protein homeostasis, tetramer, α-synuclein, Mammalian Pathological Biochemistry: Nervous System and Psychiatric Diseases and other aspects.Application of 79642-50-5

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zhang, Zhen-Yu; Wang, Qian; Hou, Ping-Ping; Shen, Zhihao; Fan, Xing-He published an article in 2015, the title of the article was Effects of rigid cores and flexible tails on the phase behaviors of polynorbornene-based mesogen-jacketed liquid crystalline polymers.Formula: C22H19NO4 And the article contains the following content:

A new series of mesogen-jacketed liquid crystalline polymers (MJLCPs) with a polynorbornene main chain and different side groups were prepared by ring-opening metathesis polymerization The liquid crystalline (LC) phase behaviors of these polymers were investigated by differential scanning calorimetry, polarized light microscopy, and wide-angle X-ray diffraction. Depending on the rigid side-chain core and peripheral alkyl chains, these polymers show different LC structures. The polymer with the terphenyl rigid side-chain core and relatively short alkyl tails is amorphous in the whole temperature range, while those with the same rigid side-chain core but longer alkyl tails exhibit columnar nematic (Coln) phases. Polymers with a longer rigid side-chain core and relatively long alkyl tails develop into smectic A (SmA) phases. In addition, the LC polymers obtained in this study display LC phases in wide temperature ranges. The experimental process involved the reaction of Dimethyl 2′-amino-[1,1′:4′,1”-terphenyl]-4,4”-dicarboxylate(cas: 1312703-30-2).Formula: C22H19NO4

The Article related to polynorbornene mesogen jacketed liquid crystalline polymer phase behavior, ring opening metathesis polymerization thermal property, Chemistry of Synthetic High Polymers: Ring-Opening and Other Polymerizations and other aspects.Formula: C22H19NO4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On August 25, 2020, Zhang, Xingxian; He, Kailun; Wang, Wenbing published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of lenalidomide derivatives as antitumor agents. And the patent contained the following:

The invention discloses a preparation of lenalidomide derivative with general formula I as antitumor agents [wherein A = (CH2CH2X)n, n = 1 to 6; X = O or CH2]. For example, compound I (n = 2, X = O) was prepared in a multi-step synthesis. The title compounds have good antitumor activity and EGFR protein degradation level, which can be used to prepare antitumor agents. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Category: esters-buliding-blocks

The Article related to substitution iodization hydrolysis amidation preparation lenalidomide pyrimidine antitumor human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On February 5, 2021, Yang, Xiaobao; Jiang, Biao; Song, Xiaoling; Sun, Ning; Ren, Chaowei; Sun, Renhong; Qu, Xiaojuan; Liu, Haixia; Qiu, Xing published a patent.Category: esters-buliding-blocks The title of the patent was Diastereoselective preparation of (aryl)amides derivatives as antitumor agents for EGFR degradation. And the patent contained the following:

The present invention relates to the diastereoselective preparation of (aryl)amides derivatives as antitumor agents for EGFR degradation In particular, (aryl)amide derivatives I [wherein, EGFR binders can bind to EGFR protein; ULM is II; wherein, A is selected from -CH2-, -(C=O)-; B, X, Y, and Z are each independently selected from CH and N; R is -S-, -SO-, -NH-, etc., or not present; D is -(C=O)-, or D does not exist; or, ULM is III, wherein, Z is selected from -(C=O)-, or Z does not exist; or, ULM is IV, wherein, A is selected from -CH2-, -NR’-, -O-, -S-, -(C=O)-, wherein R’ is selected from H, linear or branched C1-C10 alkyl or C3-C10 cycloalkyl; B is -(C=O)-, or B does not exist; D1, D2, D3, D4, D5, D6, D7, D8 are each independently selected from F, Cl, Br, etc.; LIN represents a linking group connected to EGFR binders and ULM through covalent bonds.] bifunctional compound or a pharmaceutically acceptable salt, isomer, prodrug, polymorph or solvate thereof were prepared The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Category: esters-buliding-blocks

The Article related to aryl amide derivative preparation antitumor agent egfr degradation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On September 6, 2019, Zhang, Xingxian; He, Kailun; Wang, Wenbing; Wang, Xiaoju; Zheng, Xiaoliang published a patent.HPLC of Formula: 882518-89-0 The title of the patent was Compound targeting EGFR protein degradation useful in treatment of cancer and its preparation. And the patent contained the following:

The invention relates to compounds of formula I and II targeting EGFR protein degradation useful in treatment of cancer and its preparation Compounds I and II, wherein R is C1-6 alkyl; m is an integer of 1-7; n is an integer of 1-6; their pharmaceutically acceptable salts, are claimed. The inventive compound shows excellent EGFR-degrading action and high antitumor activity, and can be applied in cancer prevention and/or treatment. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).HPLC of Formula: 882518-89-0

The Article related to pyrimidine derivative preparation treatment cancer egfr degrading, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 882518-89-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On June 28, 2018, Grew, Andrew P.; Zimmermann, Kurt; Wang, Jing; Berlin, Michael; Dong, Hanqing; Ishchenko, Alexey; Qian, Yimin; Crews, Craig M.; Jaime-Figueroa, Saul; Burslem, George published a patent.Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Preparation of heterocyclic compounds as EGFR proteolysis targeting chimeric molecules and associated methods of use. And the patent contained the following:

The disclosure relates to bifunctional compounds of formula I, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. The disclosure is directed to bifunctional compounds of formula I, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the disclosure. Compounds of formula I wherein ULM is a small mol. E3 ubiquitin ligase binding moiety; PTM is a small mol. receptor tyrosine kinase protein targeting moiety; L is a bond and a chem. linking moiety; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluate for their EGFR inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of in the range of 0.0021 μM to 12 μM. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

The Article related to heterocycle preparation egfr proteolysis targeting chimeric mol, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On July 30, 2014, Han, Xu; Bian, Shudan; Liang, Yong; Houk, K. N.; Braunschweig, Adam B. published an article.Name: Bis(2,5-dioxopyrrolidin-1-yl) glutarate The title of the article was Reactions in Elastomeric Nanoreactors Reveal the Role of Force on the Kinetics of the Huisgen Reaction on Surfaces. And the article contained the following:

The force dependence of the copper-free Huisgen cycloaddition between an alkyne and a surface-bound azide was examined in elastomeric nanoreactors. These studies revealed that pressure and chain length are critical factors that determine the reaction rate. These experiments demonstrate the central role of pressure and surface structure on interfacial processes that are increasingly important in biol., materials science, and nanotechnol. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Name: Bis(2,5-dioxopyrrolidin-1-yl) glutarate

The Article related to elastomeric nanoreactor force kinetics huisgen surface, Physical Organic Chemistry: Ring Formation, Cleavage, Enlargement, and Contraction and other aspects.Name: Bis(2,5-dioxopyrrolidin-1-yl) glutarate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Yan, Qin; Zheng, Hong-Ning; Jiang, Chuan; Li, Kun; Xiao, Shou-Jun published an article in 2015, the title of the article was EDC/NHS activation mechanism of polymethacrylic acid: anhydride versus NHS-ester.Product Details of 79642-50-5 And the article contains the following content:

Polymer brushes of poly(methacrylic acid) (PMAA) and PMAA/PNIPAM (poly-N-isopropylacrylamide) copolymers were prepared on porous silicon for further investigation of the EDC/NHS (1-ethyl-3-(3-dimethylaminopropyl)carbodiimide/N-hydroxysuccinimide) activation mechanisms by IR spectroscopy. When the fragmentation degree of PMAA blocks in the copolymer is increased, the production of anhydride wanes from dominant to recessive, whereas a complementary product of the NHS-ester waxes from recessive to dominant. The Thorpe-Ingold effect was applied to explain the formation of anhydride: the gem-dialkyl groups of PMAA next to the carboxylic acids compress the acid side chains close to each other; thus, once the intermediate of O-acylisourea forms, it will be attacked by the intramol. neighboring acid much faster than any other nucleophiles such as NHS and water, and therefore the six-membered ring of the anhydride will be formed. All acid side chains in PMAA standing next to each other will form an anhydride, primarily due to the Thorpe-Ingold effect, unless they are sterically hindered, whereas only isolated acid side chains form the NHS-ester. The EDC/NHS activation results for four small mols. of dicarboxylic acids in aqueous media, namely, glutaric acid and 2,2-di-Me glutaric acid, which generate disuccinimidyl ester with high yield, and succinic acid and 2,2-di-Me succinic acid, which remain intact, can also be explained by the Thorpe-Ingold effect. A clear understanding of the EDC/NHS activation mechanisms of PMAA will take us a step closer for resolving the mechanistic ambiguity of the carbodiimide/additive coupling reactions for amide bond formation. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Product Details of 79642-50-5

The Article related to ethyldimethylaminopropylcarbodiimide hydroxysuccinimide activation mechanism polymethacrylic acid anhydride, Chemistry of Synthetic High Polymers: Monomers and Reagents Used In Polymerization and other aspects.Product Details of 79642-50-5

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 21, 2000, Alstermark, Christer; Andersson, Kjell; Bjore, Annika; Bjorsne, Magnus; Lindstedt, Alstermark Eva-Lotte; Nilsson, Goran; Polla, Magnus; Strandlund, Gert; Ortengren, Ylva published a patent.COA of Formula: C19H26N2O3 The title of the patent was Preparation of new bispidines useful in the treatment of cardiac arrhythmias. And the patent contained the following:

Bispidines, such as I [R3 = H, alkyl; R4 = H, alkyl, alkoxy; NR3R4 = heterocyclyl; R5 = H, halogen, alkyl, alkoxy, acyloxy, alkylsulfonyloxy, carbamoyl, etc.; R6 = H, alkyl; R5R6 = O; R7 = alkyl, aryl, heterocyclyl; A, B = bond, linking group, such as alkylene, etc.], were prepared for pharmaceutical use in the treatment of cardiac arrhythmias, in particular atrial and ventricular arrhythmias. Thus, bispidine II was prepared with 51% yield by amidation of (S)-4-[3-(3,7-diazabicyclo[3.3.1]non-3-yl)-2-hydroxypropoxy]benzonitrile with Et isocyanate. The prepared bispidines were tested for primary electrophysiol. effects in anesthetized guinea pigs. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).COA of Formula: C19H26N2O3

The Article related to bispidine preparation cardiac arrhythmia treatment, antiarrhythmic bispidine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.COA of Formula: C19H26N2O3

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 21, 2000, Bjore, Annika; Bjorsne, Magnus; Halvarsson, Torbjorn; Hoffmann, Kurt-jurgen; Samuelsson, Bertil; Strandlund, Gert published a patent.Electric Literature of 227940-70-7 The title of the patent was Preparation of new bispidines useful in the treatment of cardiac arrhythmias. And the patent contained the following:

Bispidines, such as I [R1 = alkyl, arylalkyl, etc.; R2, R3 = H, OH, alkyl, etc.; R2R3 = O; R4, R5a, R5b = H, alkyl; R6 = OH, CN, NO2, NH2, halogen, etc.; X = O, S; A, B = bond, linking group, such as alkylene, etc.; D = H, OH, alkyl, aminoalkyl, etc.], were prepared for pharmaceutical use in the treatment of cardiac arrhythmias, in particular atrial and ventricular arrhythmias. Thus, bispidine II was prepared in multistep synthetic sequence starting from Et 4-oxo-1-piperidinecarboxylate, epichlorohydrin, and 4-cyanophenol. The prepared bispidines were tested for primary electrophysiol. effects in anesthetized guinea pigs. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Electric Literature of 227940-70-7

The Article related to bispidine preparation cardiac arrhythmia treatment, antiarrhythmic bispidine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Electric Literature of 227940-70-7

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics