Tag: M.W=250-300

Wu, Shaotong published the artcileA stereo configuration-activity study of 3-iodo-4-(2-methylcyclohexyloxy)-6-phenethylpyridin-2(2H)-ones as potency inhibitors of HIV-1 variants, HPLC of Formula: 21286-54-4, the publication is Organic & Biomolecular Chemistry (2016), 14(4), 1413-1420, database is CAplus and MEDLINE.

3-Iodo-4-(2′-methylcyclohexyloxy)-6-phenethylpyridin-2(1H)-ones, as effective non-nucleoside reverse transcriptase inhibitors, were synthesized and resolved with different configurations. Biol. results revealed that the trans-racemate exhibited more potent activity than the cis-isomers. Noticeably, the trans-(S,S)-enantiomer turned out to be significantly more potent than its counterpart enantiomer against wild-type and double-mutant strains with high selectivity indexes.

Organic & Biomolecular Chemistry published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C11H9NO3, HPLC of Formula: 21286-54-4.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kornecook, Thomas J. published the artcilePharmacologic characterization of AMG8379, a potent and selective small molecule sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, HPLC of Formula: 929626-16-4, the publication is Journal of Pharmacology and Experimental Therapeutics (2017), 362(1), 146-160, database is CAplus and MEDLINE.

Potent and selective antagonists of the voltage-gated sodium channel NaV1.7 represent a promising avenue for the development of new chronic pain therapies. We generated a small mol. atropisomer quinolone sulfonamide antagonist AMG8379 and a less active enantiomer AMG8380. Here we show that AMG8379 potently blocks human NaV1.7 channels with an IC50 of 8.5 nM and endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with an IC50 of 3.1 nM in whole-cell patch clamp electrophysiol. assays using a voltage protocol that interrogates channels in a partially inactivated state. AMG8379 was 100- to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in the heart, as well as TTX-resistant NaV channels in DRG neurons. Using an ex vivo mouse skin-nerve preparation, AMG8379 blocked mech. induced action potential firing in C-fibers in both a time-dependent and dose-dependent manner. AMG8379 similarly reduced the frequency of thermally induced C-fiber spiking, whereas AMG8380 affected neither mech. nor thermal responses. In vivo target engagement of AMG8379 in mice was evaluated in multiple NaV1.7-dependent behavioral endpoints. AMG8379 dose-dependently inhibited intradermal histamine-induced scratching and intraplantar capsaicin-induced licking, and reversed UVB radiation skin burn-induced thermal hyperalgesia; notably, behavioral effects were not observed with AMG8380 at similar plasma exposure levels. AMG8379 is a potent and selective NaV1.7 inhibitor that blocks sodium current in heterologous cells as well as DRG neurons, inhibits action potential firing in peripheral nerve fibers, and exhibits pharmacodynamic effects in translatable models of both itch and pain.

Journal of Pharmacology and Experimental Therapeutics published new progress about 929626-16-4. 929626-16-4 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronate Esters, name is 2-(3-Chloro-5-methoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, and the molecular formula is C13H18BClO3, HPLC of Formula: 929626-16-4.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kornecook, Thomas J. published the artcilePharmacologic characterization of AMG8379, a potent and selective small molecule sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, Quality Control of 960388-56-1, the publication is Journal of Pharmacology and Experimental Therapeutics (2017), 362(1), 146-160, database is CAplus and MEDLINE.

Potent and selective antagonists of the voltage-gated sodium channel NaV1.7 represent a promising avenue for the development of new chronic pain therapies. We generated a small mol. atropisomer quinolone sulfonamide antagonist AMG8379 and a less active enantiomer AMG8380. Here we show that AMG8379 potently blocks human NaV1.7 channels with an IC50 of 8.5 nM and endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with an IC50 of 3.1 nM in whole-cell patch clamp electrophysiol. assays using a voltage protocol that interrogates channels in a partially inactivated state. AMG8379 was 100- to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in the heart, as well as TTX-resistant NaV channels in DRG neurons. Using an ex vivo mouse skin-nerve preparation, AMG8379 blocked mech. induced action potential firing in C-fibers in both a time-dependent and dose-dependent manner. AMG8379 similarly reduced the frequency of thermally induced C-fiber spiking, whereas AMG8380 affected neither mech. nor thermal responses. In vivo target engagement of AMG8379 in mice was evaluated in multiple NaV1.7-dependent behavioral endpoints. AMG8379 dose-dependently inhibited intradermal histamine-induced scratching and intraplantar capsaicin-induced licking, and reversed UVB radiation skin burn-induced thermal hyperalgesia; notably, behavioral effects were not observed with AMG8380 at similar plasma exposure levels. AMG8379 is a potent and selective NaV1.7 inhibitor that blocks sodium current in heterologous cells as well as DRG neurons, inhibits action potential firing in peripheral nerve fibers, and exhibits pharmacodynamic effects in translatable models of both itch and pain.

Journal of Pharmacology and Experimental Therapeutics published new progress about 960388-56-1. 960388-56-1 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronate Esters,Boronic Acids,Boronic acid and ester,Boronate Esters, name is 3-Chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol, and the molecular formula is C12H16BClO3, Quality Control of 960388-56-1.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Lu, Xu published the artcileHydrogen Bond-Accelerated meta-Selective C-H Borylation of Aromatic Compounds and Expression of Functional Group and Substrate Specificities, Safety of Methyl 3-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, the publication is ACS Catalysis (2019), 9(3), 1705-1709, database is CAplus.

Meta-selective C-H borylation of aromatic compounds was accelerated when using urea moiety-containing bipyridine-type ligands unlike in cases involving a bipyridine-type ligand without the urea moiety. The acceleration was due to the recognition and capture of the aromatic substrates by the urea moiety of the ligand by H bonding. The acceleration was further enhanced by modifying the electronic and steric properties of the ligand. The functional group and substrate specificities were also observed using the urea moiety-containing ligands.

ACS Catalysis published new progress about 408492-29-5. 408492-29-5 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ester,Boronate Esters,Boronate Esters,Boronic acid and ester,, name is Methyl 3-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, and the molecular formula is C14H18BClO4, Safety of Methyl 3-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Wang, Bin published the artcileTBN-mediated regio- and stereoselective sulfonylation & oximation (oximosulfonylation) of alkynes with sulfonyl hydrazines in EtOH/H₂O, Formula: C7H3Cl2F3O2S, the publication is Green Chemistry (2019), 21(2), 205-212, database is CAplus.

Terminal aryl alkynes such as phenylacetylene underwent regioselective and diastereoselective cascade sulfonylation and oximation reactions with arylsulfonyl hydrazides such as 4-MeC₆H₄SO₂NHNH₂ mediated by tert-Bu nitrite (TBN), hydrazine hydrate, and imidazole in 40:1 EtOH:H₂O to yield (Z)-α-sulfonyl aryl Me ketoximes such as (Z)-4-MeC₆H₄SO₂CH₂C(:NOH)Ph. The mechanism was studied through identification of byproducts and radical inhibition and deuterium incorporation studies.

Green Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C4H6O3, Formula: C7H3Cl2F3O2S.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kou, Wen-Ting published the artcilePost-synthetic modification of metal-organic frameworks for chiral gas chromatography, Name: ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, the publication is Journal of Materials Chemistry A: Materials for Energy and Sustainability (2018), 6(37), 17861-17866, database is CAplus.

Chiral metal-organic frameworks (MOFs) show great potential in chiral catalysis and separation However, their application is still hindered by the limited availability of chiral MOFs and chiral recognition centers due to the great challenges for direct synthesis of chiral MOFs with designed chiral recognition sites. Here we report a post-synthesis approach for the facile preparation of chiral MOFs for chiral gas chromatog. Five chiral MOFs with an identical parent framework but different chiral recognition sites were synthesized via grafting various chiral recognition sites of ligands onto MIL-101-NH₂. The chiral MOF-coated capillary columns gave good resolution for the separation of diverse racemates with superior separation to the com. chiral capillary columns. The results reveal that the post-synthesis approach is convenient to fabricate target chiral MOFs with pre-designed functions with the ability to avoid blind synthesis of chiral MOFs via direct synthesis and to facilitate the evolution of chiral stationary phases in chiral chromatog.

Journal of Materials Chemistry A: Materials for Energy and Sustainability published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C10H15ClO3S, Name: ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kok, Germaine Pui Yann published the artcileCu-Catalyzed [3 + 3] Cycloaddition of Isocyanoacetates with Aziridines and Stereoselective Access to α,γ-Diamino Acids, Name: Sodium chloro(tosyl)amide trihydrate, the publication is Organic Letters (2018), 20(17), 5112-5115, database is CAplus and MEDLINE.

We report herein an efficient Cu-catalyzed formal [3 + 3] cycloaddition of isocyanoacetates with readily available aziridines of different substitution patterns, which provides a practical access to valuable 1,4,5,6-tetrahydropyrimidine derivatives In particular, the use of enantiopure aziridines delivers disubstituted tetrahydropyrimidines bearing a 1,3-diamino unit in good yields as a single stereoisomer (>20:1 dr, > 99% ee). The heterocyclic products can also be easily converted to synthetically useful amino alc. derivatives or α,γ-diamino acids.

Organic Letters published new progress about 7080-50-4. 7080-50-4 belongs to chlorides-buliding-blocks, auxiliary class Halogenation Reagent,Inhibitor, name is Sodium chloro(tosyl)amide trihydrate, and the molecular formula is C7H13ClNNaO5S, Name: Sodium chloro(tosyl)amide trihydrate.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Luo, Zhan-gang published the artcileDetermination of total cyanide in water by flow injection, Synthetic Route of 7080-50-4, the publication is Zhongguo Weisheng Jianyan Zazhi (2012), 22(7), 1510-1511, database is CAplus.

The objective of this paper is to establish a method for detection of total cyanide in water by flow injection. In this study, FSIV + flow injection was selected. The sample was decomposed in an acidic medium by UV-light. The hydrogen cyanide was separated by online distillation at 160 °C. The hydrogen cyanide reacted with chloramine T trihydrate while pH â‰?8 to produce hydrogen chloride, which reacted with pyridine-barbituric acid to give a red complex for detection at wavelength of 570 nm. Results show that this method had a good correlation (r>0.9990, n=6), the RSD% of standards and samples were both less than 5%. The spike recovery rate in samples was between 87% and 105% and the method detection limit was 0.97 μg/L. It was concluded that the method is rapid, accurate, highly sensitive and the results are satisfactory.

Zhongguo Weisheng Jianyan Zazhi published new progress about 7080-50-4. 7080-50-4 belongs to chlorides-buliding-blocks, auxiliary class Halogenation Reagent,Inhibitor, name is Sodium chloro(tosyl)amide trihydrate, and the molecular formula is C7H13ClNNaO5S, Synthetic Route of 7080-50-4.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Zhang, Wenwen published the artcileMicrodroplets as Microreactors for Fast Synthesis of Ketoximes and Amides, Related Products of chlorides-buliding-blocks, the publication is Journal of Organic Chemistry (2019), 84(2), 851-859, database is CAplus and MEDLINE.

The formation of amide bonds is one of the most valuable transformations in organic synthesis. Beckmann rearrangement is a well-known method for producing secondary amides from ketoximes. This study demonstrates the rapid synthesis of ketoximes and amides in microdroplets. Many factors are found to affect the yield, such as microdroplet generation devices, temperature, catalysts, and concentrations of reactants. In particular, the temperature has a great influence on the synthesis of amide, which is demonstrated by a sharp ascendance to the yield when the temperature was increased to 45°. The best amide yield (93.3%) can be obtained by using coaxial flowing devices, a sulfonyl chloride compound as a catalyst, and heating to 55° in microdroplets. The yields can reach 78.7-91.3% for benzoylaniline and 87.2-93.4% for benzophenone oximes in several seconds in microdroplets compared to 10.1-66.1% and 82.5-93.3% in several hours in the bulk phase. Apart from the dramatically decreased reaction time and enhanced reaction yields, the microdroplet synthesis is also free of severe reaction environments (anhydrous and anaerobic conditions). In addition, the synthesis in microdroplets also saves reactants and solvents and reduces the waste amounts All of these merits indicate that the microdroplet synthesis is a high-efficiency green methodol.

Journal of Organic Chemistry published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C11H15NOS, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Usui, Kazuteru published the artcileSynthesis and Resolution of Substituted [5]Carbohelicenes, Related Products of chlorides-buliding-blocks, the publication is Journal of Organic Chemistry (2015), 80(12), 6502-6508, database is CAplus and MEDLINE.

Three types of racemic [5]helicenyl acetates [I (R = Ac), II, and III (R = Ac)] were synthesized. The synthesis of II was achieved by regioselective oxidation using o-iodoxybenzoic acid. The enzymic kinetic resolution of I–III (R = Ac) was studied. The conversion with the highest rate and ee was obtained using I (R = Ac) as the substrate and lipase Amano PS-IM as the enzyme. The two enantiomers of 1-[5]helicenol III (R = H) were separated using (1S)-10-camphorsulfonyl chloride as the chiral resolving agent.

Journal of Organic Chemistry published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C14H21BO3S, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics