Shafiee, A.’s team published research in Journal of Pharmaceutical Sciences in 72 | CAS: 101-98-4

Journal of Pharmaceutical Sciences published new progress about 101-98-4. 101-98-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Alcohol, name is 2-(Benzyl(methyl)amino)ethanol, and the molecular formula is C12H23N3S, Name: 2-(Benzyl(methyl)amino)ethanol.

Shafiee, A. published the artcileSynthesis and pharmacological activity of benzo[b]thiophene-3-carboxylic acid derivatives, Name: 2-(Benzyl(methyl)amino)ethanol, the publication is Journal of Pharmaceutical Sciences (1983), 72(2), 198-202, database is CAplus and MEDLINE.

Benzothiophenes I (R = amino, aminoalkyl) and II (R1 = aminoalkoxy, amino) were prepared from I (R = Cl, N3) resp. I (R = Me2NCH2CH2) showed significant anticholinergic and antihistamine activity at 1 μg/mL whereas I (R = Me2NCMe2CH2, morpholinoethyl) showed local anesthetic activity comparable to that of lidocaine HCl.

Journal of Pharmaceutical Sciences published new progress about 101-98-4. 101-98-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Alcohol, name is 2-(Benzyl(methyl)amino)ethanol, and the molecular formula is C12H23N3S, Name: 2-(Benzyl(methyl)amino)ethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Creary, Xavier’s team published research in Journal of Organic Chemistry in 80 | CAS: 20117-47-9

Journal of Organic Chemistry published new progress about 20117-47-9. 20117-47-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic cyclic hydrocarbon,Alcohol, name is 1-Methylcyclobutan-1-ol, and the molecular formula is C5H10O, COA of Formula: C5H10O.

Creary, Xavier published the artcileγ-Trimethylsilylcyclobutyl Carbocation Stabilization, COA of Formula: C5H10O, the publication is Journal of Organic Chemistry (2015), 80(3), 1781-1788, database is CAplus and MEDLINE.

Isomeric 3-trimethylsilyl-1-arylcyclobutyl carbocations, where the cross-ring 3-trimethylsilyl group has the potential to interact with the cationic center, were generated under solvolytic conditions. When the cationic center can interact with the rear lobe of the carbon-silicon bond, rate enhancements become progressively larger as the substituent on the aryl group becomes more electron-withdrawing. When the potential interaction with the trimethylsilyl group is via a front lobe interaction, there is minimal rate enhancement over the range of substituents. Computational studies also were carried out on these cations. Calculated trimethylsilyl stabilization energies progressively increase with electron-withdrawing character of the aryl groups when the trimethylsilyl interaction is via the rear lobe. But there are minimal changes in stabilization energies when the potential trimethylsilyl interaction is via the front lobe of the carbon-silicon bond. These computational studies, along with the solvolytic studies, point to a significant rear lobe 3-trimethylsilyl stabilization of arylcyclobutyl cations. They also argue against any front lobe stabilization of the isomeric arylcyclobutyl cations.

Journal of Organic Chemistry published new progress about 20117-47-9. 20117-47-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic cyclic hydrocarbon,Alcohol, name is 1-Methylcyclobutan-1-ol, and the molecular formula is C5H10O, COA of Formula: C5H10O.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Musdal, Yaman’s team published research in Chemico-Biological Interactions in 205 | CAS: 3818-50-6

Chemico-Biological Interactions published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, HPLC of Formula: 3818-50-6.

Musdal, Yaman published the artcileFDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1, HPLC of Formula: 3818-50-6, the publication is Chemico-Biological Interactions (2013), 205(1), 53-62, database is CAplus and MEDLINE.

Glutathione transferase P1-1 (GST P1-1) is often overexpressed in tumor cells and is regarded as a contributor to their drug resistance. Inhibitors of GST P1-1 are expected to counteract drug resistance and may therefore serve as adjuvants in the chemotherapy of cancer by increasing the efficacy of cytostatic drugs. Finding useful inhibitors among compounds used for other indications would be a shortcut to clin. applications and a search for GST P1-1 inhibitors among approved drugs and other compounds was therefore conducted. We tested 1040 FDA-approved compounds as inhibitors of the catalytic activity of purified human GST P1-1 in vitro. We identified chlorophyllide, merbromine, hexachlorophene, and ethacrynic acid as the most effective GST P1-1 inhibitors with IC50 values in the low micromolar range. For comparison, these compounds were even more potent in the inhibition of human GST A3-3, an enzyme implicated in steroid hormone biosynthesis. In distinction from the other inhibitors, which showed conventional inhibition patterns, the competitive inhibitor ethacrynic acid elicited strong kinetic cooperativity in the glutathione saturation of GST P1-1. Apparently, ethacrynic acid serves as an allosteric inhibitor of the enzyme. In their own right, the compounds investigated are less potent than desired for adjuvants in cancer chemotherapy, but the structures of the most potent inhibitors could serve as leads for the synthesis of more efficient adjuvants.

Chemico-Biological Interactions published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, HPLC of Formula: 3818-50-6.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Willwacher, Jens’s team published research in Chemistry – A European Journal in 21 | CAS: 57044-25-4

Chemistry – A European Journal published new progress about 57044-25-4. 57044-25-4 belongs to alcohols-buliding-blocks, auxiliary class Epoxides,Chiral,Aliphatic hydrocarbon chain,Alcohol, name is (R)-Oxiran-2-ylmethanol, and the molecular formula is C15H20O6, Product Details of C3H6O2.

Willwacher, Jens published the artcileTotal Synthesis, Stereochemical Revision, and Biological Reassessment of Mandelalide A: Chemical Mimicry of Intrafamily Relationships, Product Details of C3H6O2, the publication is Chemistry – A European Journal (2015), 21(29), 10416-10430, database is CAplus and MEDLINE.

Mandelalide A and three congeners had recently been isolated as the supposedly highly cytotoxic principles of an ascidian collected off the South African coastline. Since these compounds are hardly available from the natural source, a concise synthesis route was developed, targeting one structure as the purported representation of mandelalide A. The sequence involves an iridium-catalyzed two-directional Krische allylation and a cobalt-catalyzed carbonylative epoxide opening as entry points for the preparation of the major building blocks. The final stages feature the first implementation of terminal acetylene metathesis into natural product total synthesis, which is remarkable in that this class of substrates had been beyond the reach of alkyne metathesis for decades. Synthetic mandelalide A, however, proved not to be identical with the natural product. In an attempt to clarify this issue, NMR spectra were simulated for 20 conceivable diastereomers by using DFT followed by DP4 anal.; however, this did not provide a reliable assignment either. The puzzle was ultimately solved by the preparation of three diastereomers, of which one compound proved identical with mandelalide A in all anal. and spectroscopic regards. As the entire northern sector about the THF ring in that compound shows the opposite configuration of what had originally been assigned, it is highly likely that the stereostructures of the sister compounds mandelalides B-D must be corrected analogously; we propose that these natural products are accurately represented by addnl. structures. In an attempt to prove this reassignment, an entry into mandelalides C and D was sought by subjecting an advanced intermediate of the synthesis of 6 to a largely unprecedented intramol. Morita-Baylis-Hillman reaction, which furnished the γ-lactone derivative 74 as a mixture of diastereomers. Whereas (24R)-74 was amenable to a hydroxyl-directed dihydroxylation by using OsO4/TMEDA as the reagent, the sister compound (24S)-74 did not follow a directed path but simply obeyed Kishi’s rule; only this unexpected escape precluded the preparation of mandelalides C and D by this route. A combined spectroscopic and computational (DFT) study showed that the reasons for this strikingly different behavior of the two diastereomers are rooted in their conformational peculiarities. This aspect apart, our results show that the OsO4/TMEDA complex reacts preferentially with electron deficient double bonds even if other alkenes are present that are more electron rich and less encumbered. Finally, in a brief biol. survey authentic mandelalide A was found to exhibit appreciable cytotoxicity only against one out of three tested human cancer cell lines and all synthetic congeners were hardly active. No significant fungicidal properties were observed The proposed new structure was (1R,3R,4E,6Z,9R,10R,12R,13R,15R,18E,21S,23R)-23-[(6-deoxy-2-O-methyl-α-L-mannopyranosyl)oxy]-13-hydroxy-15-(hydroxymethyl)-3,10-dimethyl-16,25,26-trioxatricyclo[19.3.1.19,12]hexacosa-4,6,18-trien-17-one for mandelalide A.

Chemistry – A European Journal published new progress about 57044-25-4. 57044-25-4 belongs to alcohols-buliding-blocks, auxiliary class Epoxides,Chiral,Aliphatic hydrocarbon chain,Alcohol, name is (R)-Oxiran-2-ylmethanol, and the molecular formula is C15H20O6, Product Details of C3H6O2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Remonen, Tommi’s team published research in Synthetic Metals in 101 | CAS: 239075-02-6

Synthetic Metals published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Recommanded Product: 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene.

Remonen, Tommi published the artcileEthylenedithio end-capped oligothiophenes (bEDTnT); dimer, trimer and tetramer, Recommanded Product: 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, the publication is Synthetic Metals (1999), 101(1-3), 107-108, database is CAplus.

Two new ethylenedithio substituted thiophenes (I; R = H, Br) have been synthesized. Starting from I (R = Br), oligomers II (n = 0, 1, 2) were synthesized. Their cyclic voltammetric behavior and electronic structure (by UV-Vis) have been recorded. Low oxidation potentials and small differences between first and second oxidation potential were found. In the UV-Vis spectra large red shifts compared to other end-capped oligomers were observed

Synthetic Metals published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Recommanded Product: 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Del Grosso, Alessandro’s team published research in Chemical Communications (Cambridge, United Kingdom) in 47 | CAS: 239075-02-6

Chemical Communications (Cambridge, United Kingdom) published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Computed Properties of 239075-02-6.

Del Grosso, Alessandro published the artcileSimple inexpensive boron electrophiles for direct arene borylation, Computed Properties of 239075-02-6, the publication is Chemical Communications (Cambridge, United Kingdom) (2011), 47(46), 12459-12461, database is CAplus and MEDLINE.

Borenium ions, stabilized by coordination of hindered aromatic amines, were shown to act as reactive electrophiles for direct borylation of activated arenes and heterocyclic compounds, such as indoles and thiophenes. 2,6-Lutidine complex of dichloroborenium, [2,6-Me2C5H3N·BCl2][AlCl4] was isolated and characterized by single-crystal x-ray diffraction, featuring low degree of π-bonding and high electrophilicity. Friedel-Crafts-type reaction of ArH with BCl3, catalyzed by AlCl3 in the presence of N,N-dimethyltoluidine or 2,6-lutidine as borenium stabilizing agents, followed by esterification with 2.2-3 equiv of pinacol, gave pinacolboronates ArBpin (Ar = 1-TIPS-3-pyrrolyl, 1-methyl-3-indolyl, 2,2′-bithiophen-5-yl, thieno[3,2-b]thien-2-yl, 4-(phenyl)(p-tolyl)aminophenyl, etc.). Electrophilic direct borylation is facilitated, and arene substrate scope enhanced, by using electrophiles derived from inexpensive reagents; specifically an amine, BCl3 and AlCl3.

Chemical Communications (Cambridge, United Kingdom) published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Computed Properties of 239075-02-6.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Forcellini, Elsa’s team published research in Journal of Fluorine Chemistry in 180 | CAS: 83706-94-9

Journal of Fluorine Chemistry published new progress about 83706-94-9. 83706-94-9 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is (E)-4,4,4-Trifluorobut-2-en-1-ol, and the molecular formula is C4H5F3O, Formula: C4H5F3O.

Forcellini, Elsa published the artcileSystematic study of the reactivity of (E)-4,4,4-trifluorobut-2-en-1-yl 4-methylbenzenesulfonate towards different classes of nucleophiles, Formula: C4H5F3O, the publication is Journal of Fluorine Chemistry (2015), 216-221, database is CAplus.

The alkylation of 4-phenylphenol, benzyl alc., thiols, primary and secondary amines, indole, and malonates by (E)-F3CCH:CHCH2OTs was studied; in most cases (4-phenylphenol, thiols, amines, malonates), alkylation of the nucleophiles was most effective using K2CO3 in MeCN, while none of the conditions tried were effective for indole and benzyl alc.

Journal of Fluorine Chemistry published new progress about 83706-94-9. 83706-94-9 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is (E)-4,4,4-Trifluorobut-2-en-1-ol, and the molecular formula is C4H5F3O, Formula: C4H5F3O.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Lee, Sie Huey’s team published research in International Journal of Pharmaceutics (Amsterdam, Netherlands) in 572 | CAS: 23828-92-4

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Application In Synthesis of 23828-92-4.

Lee, Sie Huey published the artcileInhaled mucoactive particles with tailored architecture for enhanced aerodynamicity, stability and efficacy, Application In Synthesis of 23828-92-4, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2019), 118740, database is CAplus and MEDLINE.

In respiratory and genetic disorders such as asthma, chronic obstructive pulmonary disease (COPD), chronic bronchitis and cystic fibrosis (CF), the lungs produce excess mucus, resulting in a thickened mass, which clogs up the airways and reduces airflow. Consequently, breathing becomes more difficult. Medications that break down the structure of mucus will be especially useful in managing the early symptoms of these diseases and preventing their progression into the more severe forms. This work therefore seeks to develop an inhaled mucoactive dry powder formulation that is efficacious on multiple fronts. As an innovative step, sodium chloride was used to tailor the surface architecture of ambroxol hydrochloride particles, such that the resulting angular features on the surfaces contributed to the creation of corrugated particles with enhanced aerodynamicity. The optimized spray-dried powder particles were of respirable-size (d50 of 2.85 ± 0.15 μm) and moderately corrugated. When the crystalline powder was dispersed via an Aerolizer inhaler at 60 L/min, it gave a fine particle fraction (FPF) of ∼31%, which was a ten-fold improvement over the unmodified species (i.e. ambroxol hydrochloride alone). Tests on artificial sputum medium (ASM) showed that the optimized formulation was potentially useful in liquefying the mucus, which favorably pointed towards the effectiveness of the formulation. In addition, the formulation was also stable to moisture ingress (up to ∼60% RH) and had good flowability. Hence, the advent of angular adjuvant sodium chloride particles in a mucoactive formulation conferred a three-fold benefit to the product: (1) Improved aerodynamicity and flowability, (2) Enhanced moisture stability and (3) Synergistic mucolytic properties.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Application In Synthesis of 23828-92-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Sams, Anette G.’s team published research in Journal of Medicinal Chemistry in 53 | CAS: 55346-97-9

Journal of Medicinal Chemistry published new progress about 55346-97-9. 55346-97-9 belongs to alcohols-buliding-blocks, auxiliary class Fluoride,Nitro Compound,Benzene,Phenol, name is 4,5-Difluoro-2-nitrophenol, and the molecular formula is C6H3F2NO3, Related Products of alcohols-buliding-blocks.

Sams, Anette G. published the artcileDiscovery of N-{1-[3-(3-Oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): An Allosteric Muscarinic M1 Receptor Agonist with Unprecedented Selectivity and Procognitive Potential, Related Products of alcohols-buliding-blocks, the publication is Journal of Medicinal Chemistry (2010), 53(17), 6386-6397, database is CAplus and MEDLINE.

The discovery and structure-activity relationship (SAR) of a series of allosteric muscarinic M1 receptor agonists are described. Compound 17 (Lu AE51090) was identified as a representative compound from the series, based on its high selectivity as an agonist at the muscarinic M1 receptor across a panel of muscarinic receptor subtypes. Furthermore, 17 displayed a high degree of selectivity when tested in a broad panel of G-protein-coupled receptors, ion channels, transporters, and enzymes, and 17 showed an acceptable pharmacokinetic profile and sufficient brain exposure in rodents in order to characterize the compound in vivo. Hence, in a rodent model of learning and memory, 17 reversed delay-induced natural forgetting, suggesting a procognitive potential of 17.

Journal of Medicinal Chemistry published new progress about 55346-97-9. 55346-97-9 belongs to alcohols-buliding-blocks, auxiliary class Fluoride,Nitro Compound,Benzene,Phenol, name is 4,5-Difluoro-2-nitrophenol, and the molecular formula is C6H3F2NO3, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Duclos, Marie-Christine’s team published research in ChemSusChem in 11 | CAS: 70445-33-9

ChemSusChem published new progress about 70445-33-9. 70445-33-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic Chain, name is 3-((2-Ethylhexyl)oxy)propane-1,2-diol, and the molecular formula is C11H24O3, Formula: C11H24O3.

Duclos, Marie-Christine published the artcileMethylation of Polyols with Trimethylphosphate in the Presence of a Lewis or Bronsted Acid Catalyst, Formula: C11H24O3, the publication is ChemSusChem (2018), 11(3), 547-551, database is CAplus and MEDLINE.

The alkylation of alcs. and polyols has been investigated with alkyl phosphates in the presence of a Lewis or Bronsted acid catalyst. The permethylation of polyols was developed under solvent-free conditions at 100 °C with either iron triflate or Aquivion PW98, affording the isolated products in yields between 52 and 95 %. The methodol. was also adjusted to carry out peralkylation with longer alkyl chains.

ChemSusChem published new progress about 70445-33-9. 70445-33-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic Chain, name is 3-((2-Ethylhexyl)oxy)propane-1,2-diol, and the molecular formula is C11H24O3, Formula: C11H24O3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts