Month: October 2022

Vaughan, Hannah J.; Zamboni, Camila G.; Radant, Nicholas P.; Bhardwaj, Pranshu; Revai Lechtich, Esther; Hassan, Laboni F.; Shah, Khalid; Green, Jordan J. published an article in 2021. The article was titled 《Poly(beta-amino ester) nanoparticles enable tumor-specific TRAIL secretion and a bystander effect to treat liver cancer》, and you may find the article in Molecular Therapy–Oncolytics.Recommanded Product: 156-87-6 The information in the text is summarized as follows:

Despite initial promise, tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-based approaches to cancer treatment have yet to yield a clin. approved therapy, due to delivery challenges, a lack of potency, and drug resistance. To address these challenges, we have developed poly(beta-amino ester) (PBAE) nanoparticles (NPs), as well as an engineered cDNA sequence encoding a secretable TRAIL (sTRAIL) protein, to enable reprogramming of liver cancer cells to locally secrete TRAIL protein. We show that sTRAIL initiates apoptosis in transfected cells and has a bystander effect to non-transfected cells. To address TRAIL resistance, NP treatment is combined with histone deacetylase inhibitors, resulting in >80% TRAIL-mediated cell death in target cancer cells and significantly slowed xenograft tumor growth. This anti-cancer effect is specific to liver cancer cells, with up to 40-fold higher cell death in HepG2 cancer cells over human hepatocytes. By combining cancer-specific TRAIL NPs with small-mol.-sensitizing drugs, this strategy addresses multiple challenges associated with TRAIL therapy and offers a new potential approach for cancer treatment. After reading the article, we found that the author used 3-Aminopropan-1-ol(cas: 156-87-6Recommanded Product: 156-87-6)

3-Aminopropan-1-ol(cas: 156-87-6) 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.Recommanded Product: 156-87-6

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2022,Rajput, Shruti; Kaur, Ramandeep; Jain, Nidhi published an article in Organic & Biomolecular Chemistry. The title of the article was 《Pd and photoredox dual catalysis assisted decarboxylative ortho-benzoylation of N-phenyl-7-azaindoles》.Application of 7748-36-9 The author mentioned the following in the article:

The directing group assisted decarboxylative ortho-benzoylation of N-aryl-7-azaindoles with α-keto acids was achieved by synergistic visible light promoted photoredox and palladium catalysis. The approach tenders rapid entry to aryl ketone architectures from simple α-keto acid precursors via the in situ generation of a benzoyl radical intermediate. The transformation provided a range of ortho-benzoylated N-aryl-7-azaindoles, with excellent site-selectivity and good functional group compatibility under mild reaction conditions. Biol. target predictions indicate that these mols. may serve as potential anti-cancer and anti-viral agents. In addition to this study using Oxetan-3-ol, there are many other studies that have used Oxetan-3-ol(cas: 7748-36-9Application of 7748-36-9) was used in this study.

Oxetan-3-ol(cas: 7748-36-9) is used as a reagent in the synthesis of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. It is also used as a reagent in the synthesis of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors.Application of 7748-36-9

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2022,Narjinari, Himani; Tanwar, Niharika; Kathuria, Lakshay; Jasra, Raksh Vir; Kumar, Akshai published an article in Catalysis Science & Technology. The title of the article was 《Guerbet-type β-alkylation of secondary alcohols catalyzed by chromium chloride and its corresponding NNN pincer complex》.Application of 100-55-0 The author mentioned the following in the article:

The β-alkylation of secondary alcs. had been successfully accomplished using earth abundant, inexpensive and environmentally benign 3d transition metal chromium salt CrCl3 and its corresponding pincer-Cr complex, (Ph2NNN)CrCl3 (0.005 mol%), at 140°C in air under conventional (3 h) and microwave heating conditions (ca. 75 W for 1.5 h) in the presence of NaOtBu (5 mol%) to obtain β-alkylated alcs. R(CH2)2CH(OH)R1 [R = Ph, cyclohexyl, 4-ClC6H4, etc.; R1 = Ph, 4-MeC6H4, 2-thienyl, etc.]. Microwave conditions provided better results (90% yield and 18 000 TON at 12 000 TOh-1) in comparison to conventional heating (84% yield and 16 800 TON at 5600 TOh-1). While CrCl3 (0.005 mol%) afforded 76% yield (15 200 TON at 10 133 TOh-1) of the β-alkylated alcs. under microwave conditions in the presence of 5 mol% NaOtBu, the corresponding pincer-Cr complex (Ph2NNN)CrCl3 (0.005 mol%) resulted in 90% yield (18 000 TON at 12 000 TOh-1) of the β-alkylated alcs. under similar conditions. EPR studies suggest the involvement of chromium(II) active species when either CrCl3 or its corresponding NNN pincer was used. HRMS anal., hot-filtration and mercury-drop test provided conclusive evidence for the homogeneous and well-defined mol. nature of the reaction mixture Apparently, insertion of the α-alkylated ketone into the Cr-H bond was the RDS based on inferences drawn from deuterium labeling studies that demonstrate a KIE of 7.33 and HRMS anal. which provided vital information on the resting-state of the reaction. The experimental part of the paper was very detailed, including the reaction process of 3-Pyridinemethanol(cas: 100-55-0Application of 100-55-0)

3-Pyridinemethanol(cas: 100-55-0) belongs to pyridine. Pyridine’s structure is isoelectronic with that of benzene, but its properties are quite different. Pyridine is completely miscible with water, whereas benzene is only slightly soluble. Like all hydrocarbons, benzene is neutral (in the acid–base sense), but because of its nitrogen atom, pyridine is a weak base.Application of 100-55-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2022,Saadati, Fariba; Cammarone, Silvia; Ciufolini, Marco A. published an article in Chemistry – A European Journal. The title of the article was 《A Route to Lipid ALC-0315: a Key Component of a COVID-19 mRNA Vaccine》.Recommanded Product: 4-Aminobutan-1-ol The author mentioned the following in the article:

This paper described a synthesis of ALC-0315 I by a sequence that more than doubles the overall yield relative to the published one, and that employed much cleaner reactions, thereby facilitating purifications to a considerable extent.4-Aminobutan-1-ol(cas: 13325-10-5Recommanded Product: 4-Aminobutan-1-ol) was used in this study.

4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Recommanded Product: 4-Aminobutan-1-ol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2022,Blair, Daniel J.; Chitti, Sriyankari; Trobe, Melanie; Kostyra, David M.; Haley, Hannah M. S.; Hansen, Richard L.; Ballmer, Steve G.; Woods, Toby J.; Wang, Wesley; Mubayi, Vikram; Schmidt, Michael J.; Pipal, Robert W.; Morehouse, Greg. F.; Palazzolo Ray, Andrea M. E.; Gray, Danielle L.; Gill, Adrian L.; Burke, Martin D. published an article in Nature (London, United Kingdom). The title of the article was 《Automated iterative Csp3-C bond formation》.Product Details of 821-41-0 The author mentioned the following in the article:

Fully automated synthetic chem. would substantially change the field by providing broad on-demand access to small mols. However, the reactions that can be run autonomously are still limited. Automating the stereospecific assembly of Csp3-C bonds would expand access to many important types of functional organic mols.1. Previously, methyliminodiacetic acid (MIDA) boronates were used to orchestrate the formation of Csp2-Csp2 bonds and were effective building blocks for automating the synthesis of many small mols., but they are incompatible with stereospecific Csp3-Csp2 and Csp3-Csp3 bond-forming reactions. Here authors report that hyperconjugative and steric tuning provide a new class of tetra-Me N-methyliminodiacetic acid (TIDA) boronates that are stable to these conditions. Charge d. anal. revealed that redistribution of electron d. increases covalency of the N-B bond and thereby attenuates its hydrolysis. Complementary steric shielding of carbonyl π-faces decreases reactivity towards nucleophilic reagents. The unique features of the iminodiacetic acid cage, which are essential for generalized automated synthesis, are retained by TIDA boronates. This enabled Csp3 boronate building blocks to be assembled using automated synthesis, including the preparation of natural products through automated stereospecific Csp3-Csp2 and Csp3-Csp3 bond formation. These findings will enable increasingly complex Csp3-rich small mols. to be accessed via automated assembly. In the experiment, the researchers used many compounds, for example, 5-Hexen-1-ol(cas: 821-41-0Product Details of 821-41-0)

5-Hexen-1-ol(cas: 821-41-0) is used in cyclization to a tetrahydropyran by phenylselenoetherification. It is also used as a building block in synthetic chemistry.Product Details of 821-41-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2022,Fan, You Kun; Feng, Shao Min; Liu, Xi Liang; Li, Kai Qi; Chen, Dong Liang; Xiong, Cheng Dong published an article in Macromolecular Rapid Communications. The title of the article was 《Synthesis and Characterization of Novel Radiopaque Polycarbonate》.Category: alcohols-buliding-blocks The author mentioned the following in the article:

Polymeric materials implanted in the human body are usually invisible under X-ray, and the mixing of heavy metal salts into polymeric materials by phys. compounding often poses compatibility problems. A new iodine-containing cyclic carbonate monomer, 4-iodo-N-(2-oxo-1,3-dioxan-5-yl)benzamide (IBTMC), is synthesized, which has a degradable carbonate group as its basic structural unit and iodine atoms attached to the side chain in the form of covalent bonds. The ring-opening polymerization of IBTMC is achieved at room temperature under the catalysis of the solid superbase 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD). The structure and X-ray developing ability of the synthesized polycarbonate are characterized by 1H-NMR, XPS, energy dispersive X-ray spectroscopy (EDS), Gel Permeation Chromatog. (GPC), and micro-computed tomog. (Micro-CT). The iodine atoms remain bound to the polymer as covalent bonds after a series of reactions and exhibit a high level of X-ray opacity. In vitro degradation experiments of the polymer prove that the polymer is degradable. The experimental process involved the reaction of 2-Aminopropane-1,3-diol(cas: 534-03-2Category: alcohols-buliding-blocks)

2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

HPLC of Formula: 26153-38-8In 2021 ,《Solution-processable and functionalizable ultra-high molecular weight polymers via topochemical synthesis》 appeared in Nature Communications. The author of the article were Anderson, Christopher L.; Li, He; Jones, Christopher G.; Teat, Simon J.; Settineri, Nicholas S.; Dailing, Eric A.; Liang, Jiatao; Mao, Haiyan; Yang, Chongqing; Klivansky, Liana M.; Li, Xinle; Reimer, Jeffrey A.; Nelson, Hosea M.; Liu, Yi. The article conveys some information:

Topochem. polymerization reactions hold the promise of producing ultra-high mol. weight crystalline polymers. However, the totality of topochem. polymerization reactions has failed to produce ultra-high mol. weight polymers that are both soluble and display variable functionality, which are restrained by the crystal-packing and reactivity requirements on their resp. monomers in the solid state. Herein, we demonstrate the topochem. polymerization reaction of a family of para-azaquinodimethane compounds that undergo facile visible light and thermally initiated polymerization in the solid state, allowing for the first determination of a topochem. polymer crystal structure resolved via the cryoelectron microscopy technique of microcrystal electron diffraction. The topochem. polymerization reaction also displays excellent functional group tolerance, accommodating both solubilizing side chains and reactive groups that allow for post-polymerization functionalization. The thus-produced soluble ultra-high mol. weight polymers display superior capacitive energy storage properties. This study overcomes several synthetic and characterization challenges amongst topochem. polymerization reactions, representing a critical step toward their broader application. In addition to this study using 3,5-Dihydroxybenzaldehyde, there are many other studies that have used 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8HPLC of Formula: 26153-38-8) was used in this study.

3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is a building block. It has been used in the synthesis of 2,4-dimethylbenzoylhydrazones with antileishmanial and antioxidant activities.HPLC of Formula: 26153-38-8

Referemce:
Alcohol – Wikipedia,
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Electric Literature of C4H12KNaO10In 2019 ,《Spectroscopic and theoretical studies of potassium sodium L-(+)-tartrate tetrahydrate and L-tartaric acid used as precursors for in situ laser-induced deposition of the catalytically active copper microstructures》 appeared in Optical and Quantum Electronics. The author of the article were Tumkin, Ilya I.; Khairullina, Evgeniia M.; Myund, Liubov A.; Logunov, Lev S.; Gordeychuk, Dmitrii I.; Panov, Maxim S.; Kochemirovsky, Vladimir A.. The article conveys some information:

In this work we study the influence of L-(+)-KNaC4H4O6 x 4H2O (KNaT) and L-H2C4H4O6 (H2T) on the complexation processes occurring during in situ laser-induced catalytic destruction of the organic components of the aqueous solutions with formation of the unsaturated hydrocarbons. For that purpose, ATR-FTIR, Raman, IR, and NIR spectroscopy as well as quantum chem. calculations were implemented. It was observed that hydration of T2- anion via carboxylate groups is stronger than that via hydroxyl groups. We also established the changes in the spectral characteristics of the absorption bands corresponding to vibrations of T2-, HT-, and H2T, at solid state-liquid and acid-salt transitions, depending on concentration of the solution components and the [OH-]/[H2T] ratio. Finally, it was shown that ethylene is a main product of the catalytic destruction of the copper tartrate complexes. In the experimental materials used by the author, we found Potassium sodium (2R,3R)-2,3-dihydroxysuccinate tetrahydrate(cas: 6381-59-5Electric Literature of C4H12KNaO10)

Potassium sodium (2R,3R)-2,3-dihydroxysuccinate tetrahydrate(cas: 6381-59-5) is a ferroelectric crystal with a high piezoelectric effect and electromechanical coupling coefficient. Electric Literature of C4H12KNaO10 As a Biuret reagent, it is used to measure the protein concentration. Furthermore, it is used as laxative and is also used in food industry.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Computed Properties of C6H13NOIn 2022 ,《Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase γ (PI3Kγ)》 appeared in Journal of Medicinal Chemistry. The author of the article were Mata, Guillaume; Miles, Dillon H.; Drew, Samuel L.; Fournier, Jeremy; Lawson, Kenneth V.; Mailyan, Artur K.; Sharif, Ehesan U.; Yan, Xuelei; Beatty, Joel W.; Banuelos, Jesus; Chen, Jie; Ginn, Elaine; Chen, Ada; Gerrick, Kimberline Y.; Pham, Amber T.; Wong, Kent; Soni, Divyank; Dhanota, Puja; Shaqfeh, Stefan G.; Meleza, Cesar; Narasappa, Nell; Singh, Hema; Zhao, Xiaoning; Jin, Lixia; Schindler, Ulrike; Walters, Matthew J.; Young, Stephen W.; Walker, Nigel P.; Leleti, Manmohan Reddy; Powers, Jay P.; Jeffrey, Jenna L.. The article conveys some information:

Phosphoinositide-3-kinase γ (PI3Kγ) is highly expressed in immune cells and promotes the production and migration of inflammatory mediators. The inhibition of PI3Kγ has been shown to repolarize the tumor immune microenvironment to a more inflammatory phenotype, thereby controlling immune suppression in cancer. Herein, we report the structure-based optimization of an early lead series of pyrazolopyrimidine isoindolinones, which culminated in the discovery of highly potent and isoform-selective PI3Kγ inhibitors with favorable drug-like properties. X-ray cocrystal structure anal., mol. docking studies, and detailed structure-activity relationship investigations resulted in the identification of the optimal amide and isoindolinone substituents to achieve a desirable combination of potency, selectivity, and metabolic stability. Preliminary in vitro studies indicate that inhibition of PI3Kγ with compound 56 results in a significant immune response by increasing pro-inflammatory cytokine gene expression in M1 macrophages. In the experimental materials used by the author, we found trans-4-Aminocyclohexanol(cas: 27489-62-9Computed Properties of C6H13NO)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Computed Properties of C6H13NO

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Recommanded Product: 89466-08-0In 2019 ,《Pyridinylimidazoles as GSK3β Inhibitors: The Impact of Tautomerism on Compound Activity via Water Networks》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Heider, Fabian; Pantsar, Tatu; Kudolo, Mark; Ansideri, Francesco; De Simone, Angela; Pruccoli, Letizia; Schneider, Taiane; Goettert, Marcia Ines; Tarozzi, Andrea; Andrisano, Vincenza; Laufer, Stefan A.; Koch, Pierre. The article conveys some information:

Glycogen synthase kinase-3β (GSK3β) is involved in many pathol. conditions and represents an attractive drug target. We previously reported dual GSK3β/p38α mitogen-activated protein kinase inhibitors and identified N-(4-(4-(4-fluorophenyl)-2-methyl-1H-imidazol-5-yl)pyridin-2-yl)cyclopropanecarboxamide (1) as a potent dual inhibitor of both target kinases. In this study, we aimed to design selective GSK3β inhibitors based on our pyridinylimidazole scaffold. Our efforts resulted in several novel and potent GSK3β inhibitors with IC50 values in the low nanomolar range. 5-(2-(Cyclopropanecarboxamido)pyridin-4-yl)-4-cyclopropyl-1H-imidazole-2-carboxamide (6g) displayed very good kinase selectivity as well as metabolically stability and inhibits GSK3β activity in neuronal SH-SY5Y cells. Interestingly, we observed the importance of the 2-methylimidazole’s tautomeric state for the compound activity. Finally, we reveal how this crucial tautomerism effect is surmounted by imidazole-2-carboxamides, which are able to stabilize the binding via enhanced water network interactions, regardless of their tautomeric state. In the experiment, the researchers used 2-Hydroxyphenylboronic acid(cas: 89466-08-0Recommanded Product: 89466-08-0)

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. Recommanded Product: 89466-08-0

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Alcohol – Wikipedia,
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