Tag: 100-200

Recommanded Product: 6-Aminohexan-1-olIn 2020 ,《Photoactivated Polymersome Nanomotors: Traversing Biological Barriers》 appeared in Angewandte Chemie, International Edition. The author of the article were Shao, Jingxin; Cao, Shoupeng; Williams, David S.; Abdelmohsen, Loai K. E. A.; van Hest, Jan C. M.. The article conveys some information:

Synthetic nanomotors are appealing delivery vehicles for the dynamic transport of functional cargo. Their translation toward biol. applications is limited owing to the use of non-degradable components. Furthermore, size has been an impediment owing to the importance of achieving nanoscale (ca. 100 nm) dimensions, as opposed to microscale examples that are prevalent. Herein, we present a hybrid nanomotor that can be activated by near-IR (NIR)-irradiation for the triggered delivery of internal cargo and facilitated transport of external agents to the cell. Utilizing biodegradable poly(ethylene glycol)-b-poly(D,L-lactide) (PEG-PDLLA) block copolymers, with the two blocks connected via a pH sensitive imine bond, we generate nanoscopic polymersomes that are then modified with a hemispherical gold nanocoat. This Janus morphol. allows such hybrid polymersomes to undergoing photothermal motility in response to thermal gradients generated by plasmonic absorbance of NIR irradiation, with velocities ranging up to 6.2±1.10μm s-1. These polymersome nanomotors (PNMs) are capable of traversing cellular membranes allowing intracellular delivery of mol. and macromol. cargo. In the experimental materials used by the author, we found 6-Aminohexan-1-ol(cas: 4048-33-3Recommanded Product: 6-Aminohexan-1-ol)

6-Aminohexan-1-ol(cas: 4048-33-3) can undergo cyclization over copper supported on γ-alumina and magnesia to form hexahydro-1H-azepine. It may be used along with glutaric acid to generate poly(ester amide)s with excellent film- and fiber forming properties.Recommanded Product: 6-Aminohexan-1-ol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2022,Yao, Qi-Jun; Chen, Jia-Hao; Song, Hong; Huang, Fan-Rui; Shi, Bing-Feng published an article in Angewandte Chemie, International Edition. The title of the article was 《Cobalt/Salox-Catalyzed Enantioselective C-H Functionalization of Arylphosphinamides》.COA of Formula: C9H11NO The author mentioned the following in the article:

Previous methods on Co(III)-catalyzed asym. C-H activation rely on the use of tailor-made cyclopentadienyl-ligated Co(III) complexes, which require lengthy steps for the preparation Herein, the authors report an unprecedented enantioselective C-H functionalization enabled by a simple Co/salicyloxazoline (Salox) catalysis. The chiral Salox ligands can be easily prepared in one step from salicylonitrile and chiral amino alcs. A broad range of P-stereogenic compounds were synthesized in high yields with excellent enantioselectivities (45 examples, up to 99% yield and >99% ee). The isolation and characterization of several intermediates provided insights into the generation of active catalytic Co species, the action of Salox, and the mode of stereocontrol. The experimental part of the paper was very detailed, including the reaction process of (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7COA of Formula: C9H11NO)

(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.COA of Formula: C9H11NO

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2022,Ikeda, Shuhei; Kajita, Yuichi; Miyamoto, Maki; Matsumiya, Kouta; Ishii, Tsuyoshi; Nishi, Toshiya; Gay, Sean C.; Lane, Weston; Constantinescu, Cristian C.; Alagille, David; Papin, Caroline; Tamagnan, Gilles; Kuroita, Takanobu; Koike, Tatsuki published an article in European Journal of Medicinal Chemistry. The title of the article was 《Design and synthesis of aryl-piperidine derivatives as potent and selective PET tracers for cholesterol 24-hydroxylase (CH24H)》.Recommanded Product: 18621-18-6 The author mentioned the following in the article:

Cholesterol 24-hydroxylase (CH24H, CYP46A1) is a cytochrome P 450 family enzyme that maintains the homeostasis of brain cholesterol. Soticlestat, a potent and selective CH24H inhibitor, is in development as a therapeutic agent for Dravet syndrome and Lennox-Gastaut syndrome. Herein, we report the discovery of aryl-piperidine derivatives as potent and selective CH24H positron emission tomog. (PET) tracers which can be used for dose guidance of a clin. CH24H inhibitor and as a diagnostic tool for CH24H-related pathol. Starting from compound I (IC50 = 16 nM, logD = 1.7), which was reported as a CH24H inhibitor with lower lipophilicity, a 18F-labeling site (3-fluoroazetidine) was incorporated by structure-based drug design (SBDD) utilizing the co-crystal structure of a compound I analog. Subsequent optimization to adjust key parameters for PET tracers, such as potency, lipophilicity, brain penetration, and unbound plasma protein binding, enabled compound II [Ar = 4-FC6H4, X = N] (IC50 = 8.8 nM) and compound II [Ar = 4-chloropyrazol-1-yl, X = CH] (IC50 = 8.7 nM) as PET imaging candidates. Selectivity of these compounds for CH24H was validated by a brain distribution study using CH24H-WT and KO mice. In non-human primate PET imaging, [18F] labeled analogs showed similar regional uptake in the brain, indicating that these tracers were specific to the CH24H-expressed regions and validated the expression of CH24H in the living brain by different tracers. After reading the article, we found that the author used Azetidin-3-ol hydrochloride(cas: 18621-18-6Recommanded Product: 18621-18-6)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Recommanded Product: 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wong, Siu Wai; Vivash, Lucy; Mudududdla, Ramesh; Nguyen, Nghi; Hermans, Stefan J.; Shackleford, David M.; Field, Judith; Xue, Lian; Aprico, Andrea; Hancock, Nancy C.; Haskali, Mohammad; Stashko, Michael A.; Frye, Stephen V.; Wang, Xiaodong; Binder, Michele D.; Ackermann, Uwe; Parker, Michael W.; Kilpatrick, Trevor J.; Baell, Jonathan B. published an article in 2021. The article was titled 《Development of [18F]MIPS15692, a radiotracer with in vitro proof-of-concept for the imaging of MER tyrosine kinase (MERTK) in neuroinflammatory disease》, and you may find the article in European Journal of Medicinal Chemistry.Application of 27489-62-9 The information in the text is summarized as follows:

MER tyrosine kinase (MERTK) upregulation is associated with M2 polarization of microglia, which plays a vital role in neuroregeneration following damage induced by neuroinflammatory diseases such as multiple sclerosis (MS). Therefore, a radiotracer specific for MERTK could be of great utility in the clin. management of MS, for the detection and differentiation of neuroregenerative and neurodegenerative processes. This study aimed to develop an [18F] ligand with high affinity and selectivity for MERTK as a potential positron emission tomog. (PET) radiotracer. MIPS15691 and MIPS15692 were synthesized and kinase assays were utilized to determine potency and selectivity for MERTK. Both compounds were shown to be potent against MERTK, with resp. IC50 values of 4.6 nM and 4.0 nM, and were also MERTK-selective. Plasma and brain pharmacokinetics were measured in mice and led to selection of MIPS15692 over MIPS15691. X-ray crystallog. was used to visualize how MIPS15692 is recognized by the enzyme. [18F]MIPS15692 was synthesized using an automated iPHASE FlexLab module, with a molar activity (Am) of 49 ± 26 GBq/μmol. The radiochem. purity of [18F]MIPS15692 was >99% and the decay-corrected radiochem. yields (RCYs) were determined as 2.45 ± 0.85%. Brain MERTK protein d. was measured by a saturation binding assay in the brain slices of a cuprizone mouse model of MS. High levels of specific binding of [18F]MIPS15692 to MERTK were found, especially in the corpus callosum/hippocampus (CC/HC). The in vivo PET imaging study of [18F]MIPS15692 suggested that its neuroPK is sub-optimal for clin. use. Current efforts are underway to optimize the neuroPK of our next generation PET radiotracers for maximal in vivo utility. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Application of 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Application of 27489-62-9

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ling, Huiping; Li, Hong; Chen, Meijun; Lai, Baolong; Zhou, Haiming; Gao, Hui; Zhang, Jiangye; Huang, Yan; Tao, Yiwen published an article in 2021. The article was titled 《Discovery of a Highly Potent and Novel Gambogic Acid Derivative as an Anticancer Drug Candidate》, and you may find the article in Anti-Cancer Agents in Medicinal Chemistry.SDS of cas: 627-18-9 The information in the text is summarized as follows:

Gambogic Acid (GA), a promising anti-cancer agent isolated from the resin of Garcinia species in Southeast Asia, exhibits high potency in inhibiting a wide variety of cancer cells growth. Moreover, the fact that it is amenable to chem. modification makes GA an attractive mol. for the development of anti-cancer agents. Gambogic acid-3-(4-pyrimidinyloxy) Pr ester (compound 4) was derived from the reaction between 4-hydroxypropoxy pyrimidine and GA. Its structure was elucidated by comprehensive anal. of ESIMS, HRESIMS, 1 D NMR data. Anti-tumor activities of compound 4 and GA in vitro against HepG-2, A549 and MCF-7 cells were investigated by MTT assay. FITC/PI dye was used to test apoptosis. The binding affinity difference of compound 4 and GA binding to IKKΒ was studied by using Discovery Studio 2016. Compound 4 was successfully synthesized and showed strong inhibitory effects on HepG-2, A549 and MCF-7 cells lines with an IC<> 50 value of 1.49±0.11, 1.37±0.06 and 0.64±0.16μM, resp. Mol. docking study demonstrated that four more hydrogen bonds were established between IKKΒ and compound 4, compared with GA. Our results suggested that compound 4 showed significant effects in inducing apoptosis. Further mol. docking study indicated that the introduction of pyrimidine could improve GAs binding affinity to IKKbeta. Compound 4 may serve as a potential lead compound for the development of new anti-cancer drugs. In the experiment, the researchers used 3-Bromopropan-1-ol(cas: 627-18-9SDS of cas: 627-18-9)

3-Bromopropan-1-ol(cas: 627-18-9) was used in the synthesis of fluorescent halide-sensitive quinolinium dyes and molten salt-polymers. Furthermore, it was used in the synthesis of chiral, quaternary prolines via cyclization of quaternary amino acids.SDS of cas: 627-18-9

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Muniyasamy, Harikrishnan; Chinnadurai, Chithiraikumar; Nelson, Malini; Kubendran, Aravind Manikka; Sukumaran, Karthika; Balasubramaniem, Ashokkumar; Sepperumal, Murugesan; Ayyanar, Siva; Govindasamy, Mani; Ghfar, Ayman; Alsubaied, Fehaid Mohammed published an article in 2021. The article was titled 《Highly selective flurogenic chemosensor for cyanide ion in aqueous medium and its applications of logic gate and Hela cells》, and you may find the article in Journal of Molecular Liquids.Computed Properties of C7H6O3 The information in the text is summarized as follows:

We have successfully synthesized triphenylamine-based fluorophores (MK and HK) with cyanoacrylic acid as a receptor for CN- ion sensing in a 99% aqueous medium. From the emission titration spectra, the detection limit of cyanide ion calculated toward MK and HK, resp., are 234 nM and 11 nM. The observed binding constants for MK and HK, resp., are 27 x 10-3 M and 10 X 10-2 M. The plausible sensing mechanism is confirmed by various methods such as Job′plot experiment, proton NMR titration, and d. functional theory. Furthermore, the prominent application is the naked-eye detection of cyanide from non-fluorescent to greenish-yellow fluorescent under 365 nm UV light. Based on the observed data from fluorescence spectroscopic studies, a new logic circuit is designed. Moreover, the potential application of HK and MK in the Hela cell line exhibited turn on fluorescence image for cyanide ion through the inhibition of the ICT process. In addition to that, the probe MK and HK is successfully applied in the anal. of the real sample for the rapid detection of cyanide ions. In the part of experimental materials, we found many familiar compounds, such as 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Computed Properties of C7H6O3)

3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is used as a building block in the synthesis of more complex structures. It is also used in the synthesis of terbutaline, which is an important bronchodilator.Computed Properties of C7H6O3

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Yu, Wensheng; Fells, James; Clausen, Dane; Liu, Jian; Klein, Daniel J.; Christine Chung, C.; Myers, Robert W.; Wu, Jin; Wu, Guoxin; Howell, Bonnie J.; Barnard, Richard J. O.; Kozlowski, Joseph published their research in Bioorganic & Medicinal Chemistry Letters in 2021. The article was titled 《Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation》.Product Details of 89466-08-0 The article contains the following contents:

A series of unique macrocyclic HDACs 1, 2, and 3 selective inhibitors were identified with good enzymic activity and high selectivity over HDACs 6 and 8. These macrocyclic HDAC inhibitors used an Et ketone as the zinc-binding group. Compounds I and II stood out as leads due to their low double-digit nM EC50s in the 2C4 cell-based HIV latency reactivation assay. The PK profiles of these macrocyclic HDAC inhibitors still needed improvement. In addition to this study using 2-Hydroxyphenylboronic acid, there are many other studies that have used 2-Hydroxyphenylboronic acid(cas: 89466-08-0Product Details of 89466-08-0) was used in this study.

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Product Details of 89466-08-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Qin, Haitao; Cai, Wangshui; Wang, Shuang; Guo, Ting; Li, Guigen; Lu, Hongjian published their research in Angewandte Chemie, International Edition in 2021. The article was titled 《N-Atom Deletion in Nitrogen Heterocycles》.Recommanded Product: 126456-43-7 The article contains the following contents:

A versatile method of N-atom excision from N-heterocycles was reported. The process used readily available N-heterocycles as substrates, and proceeded by N-sulfonylazidonation followed by the rearrangement of sulfamoyl azide intermediates, which provided various cyclic products. Examples were provided for deletion of nitrogen from natural products, synthesis of chiral O-heterocycles from com. available chiral β-amino alcs., formal inert C-H functionalization through a sequence of N-directed C-H functionalization and N-atom deletion reactions where the N-atom served as a traceless directing group.(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7Recommanded Product: 126456-43-7) was used in this study.

(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Recommanded Product: 126456-43-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Nelson, Hope; Richard, William; Brown, Hailee; Medlin, Abigail; Light, Christina; Heller, Stephen T. published their research in Angewandte Chemie, International Edition in 2021. The article was titled 《Practical Chemoselective Acylation: Organocatalytic Chemodivergent Esterification and Amidation of Amino Alcohols with N-Carbonylimidazoles》.Quality Control of trans-4-Aminocyclohexanol The article contains the following contents:

Here, the N-carbonylimidazoles enable catalytic chemodivergent aniline or alc. acylation in the presence of pyridinium ions or 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), was reported. Both acylation reactions display high and broad chemoselectivity for the target group. Unprecedented levels of chemoselectivity were observed in the DBU-catalyzed esterification: A single esterification product was obtained from a mol. containing primary aniline, alc., phenol, secondary amide, and N-H indole groups. These acylation reactions are highly practical as they involve only readily available, inexpensive, and relatively safe reagents; can be performed on a multigram scale; and can be used on carboxylic acids directly by in situ formation of the acylimidazole electrophile.trans-4-Aminocyclohexanol(cas: 27489-62-9Quality Control of trans-4-Aminocyclohexanol) was used in this study.

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Quality Control of trans-4-Aminocyclohexanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Palladium-Catalyzed Electrophilic Functionalization of Pyridine Derivatives through Phosphonium Salts》 was written by Che, Yuan-Yuan; Yue, Yanni; Lin, Ling-Zhi; Pei, Bingbing; Deng, Xuezu; Feng, Chao. Application In Synthesis of 3-Pyridinemethanol And the article was included in Angewandte Chemie, International Edition in 2020. The article conveys some information:

Herein, we report a highly efficient and practical method for pyridine-derived heterobiaryl synthesis through palladium-catalyzed electrophilic functionalization of easily available pyridine-derived quaternary phosphonium salts. The nice generality of this reaction was goes beyond arylation, enabling facile incorporation of diverse carbon-based fragments, including alkenyl, alkynyl, and also allyl fragments, onto the pyridine core. Notably, the silver salt additive is revealed to be of vital importance for the success of this transformation and its pivotal role as transmetallation mediator, which guarantees a smooth transfer of pyridyl group to palladium intermediate, is also described. In the experiment, the researchers used 3-Pyridinemethanol(cas: 100-55-0Application In Synthesis of 3-Pyridinemethanol)

3-Pyridinemethanol(cas: 100-55-0) belongs to pyridine. Pyridines form stable salts with strong acids. Pyridine itself is often used to neutralize acid formed in a reaction and as a basic solvent. Application In Synthesis of 3-Pyridinemethanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts