Tag: M.W=200-250

Huang, Zhuo-Bin published the artcileSelective C-H dithiocarbamation of arenes and antifungal activity evaluation, Application of 4-Iodo-1-methyl-1H-pyrazol-5-amine, the publication is Organic & Biomolecular Chemistry (2020), 18(7), 1369-1376, database is CAplus and MEDLINE.

This paper discloses a transition metal-free selective C-H dithiocarbamation of drug skeletons using disulfiram (DSF) in the presence of KI/K₂S₂O₈ in DMF/H₂O. Drug skeletons, including 5-aminopyrazoles, indoles, pyrroloquinoline, and Julolidine, underwent C-H dithiocarbamation smoothly to afford a variety of drug-like mols. in moderate to good yields. It was found that the in situ formed 5-aminopyrazole iodide is the key intermediate for the dithiocarbamation. Bioassay results show that some of these N-heterocyclic dithiocarbamate derivatives exhibit good antifungal activity against Colletotrichum gloeosprioides and Fusarium oxysporum, F. proliferatum, Fusarium solani, Geotrichum candidum, Penicillium digitatum, Penicillium italicum, Pyricularia grisea.

Organic & Biomolecular Chemistry published new progress about 1443278-79-2. 1443278-79-2 belongs to iodides-buliding-blocks, auxiliary class Pyrazole,Iodide,Amine, name is 4-Iodo-1-methyl-1H-pyrazol-5-amine, and the molecular formula is C4H6IN3, Application of 4-Iodo-1-methyl-1H-pyrazol-5-amine.

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

Dai, Lei published the artcileVisible-Light-Driven N-Heterocyclic Carbene Catalyzed γ- and ε-Alkylation with Alkyl Radicals, COA of Formula: C5H9IO2, the publication is Angewandte Chemie, International Edition (2019), 58(50), 18124-18130, database is CAplus and MEDLINE.

The merging of photoredox catalysis and N-heterocyclic carbene (NHC) catalysis for γ- and ε-alkylation of enals with alkyl radicals was developed. The alkylation reaction of γ-oxidized enals with alkyl halides worked well for the synthesis γ-multisubstituted-α,β-unsaturated esters, including those with challenging vicinal all-carbon quaternary centers. The synthesis of ε-multisubstituted-α,β-γ,δ-diunsatd. esters by an unprecedented NHC-catalyzed ε-functionalization was also established.

Angewandte Chemie, International Edition published new progress about 31253-08-4. 31253-08-4 belongs to iodides-buliding-blocks, auxiliary class Iodide,Ester, name is Ethyl 2-Iodopropionate, and the molecular formula is C5H9IO2, COA of Formula: C5H9IO2.

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

Cheng, Chaozhihui published the artcileNickel-Catalyzed Arylcarbamoylation of Alkenes of N-(o-Iodoaryl)acrylamides with Nitroarenes via Reductive Aminocarbonylation: Facile Synthesis of Carbamoyl-Substituted Oxindoles, Name: 1-Iodohexane, the publication is Organic Letters (2021), 23(24), 9543-9547, database is CAplus and MEDLINE.

Nickel-catalyzed arylcarbamoylation reactions of alkenes of N-(o-haloaryl)acrylamides with CO and nitroarenes via reductive aminocarbonylation to produce carbamoyl-substituted oxindoles with an all-carbon quaternary stereogenic center are presented. Starting with N-(o-haloaryl)acrylamides, simple CO, and inexpensive nitroarenes and using a Ni catalyst, a dinitrogen-based ligand, a Zn reductant, a TMSCl additive, and a base system, this protocol enables the synthesis of various carbamoyl-substituted oxindoles and allows the efficient late-stage derivatization of valuable mols.

Organic Letters published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C6H13I, Name: 1-Iodohexane.

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

Kuai, Chang-Sheng published the artcilePalladium-Catalyzed Regio- and Stereoselective Hydroaminocarbonylation of Unsymmetrical Internal Alkynes toward α,β-Unsaturated Amides, COA of Formula: C6H13I, the publication is Organic Letters (2022), 24(24), 4464-4469, database is CAplus and MEDLINE.

α,β-Unsaturated amides play a vital role in natural products, pharmaceuticals, organic synthesis, and functional materials. Herein, authors disclosed a regio- and stereoselective hydroaminocarbonylation of unsym. internal alkynes via palladium catalysis to synthesize α,β-unsaturated amides. This protocol features excellent regio- and exclusive (E)-stereoselectivity, high atom and step-economy, broad substrate scope, and functional group tolerance.

Organic Letters published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C6H13I, COA of Formula: C6H13I.

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

Shinohara, Mai published the artcilePhoto-control of Cellular Uptake by the Selective Adsorption of Spiropyran Derivatives on Albumin, HPLC of Formula: 638-45-9, the publication is Chemistry Letters (2022), 51(6), 594-597, database is CAplus.

A photochromic spiropyran derivative (SP6) as a drug tag was prepared SP6 was selectively taken up into cells by photo-controlling the adsorption on albumin, which has attracted attention as a carrier for delivering drugs to tumor cells. The desorption of SP6 from albumin was achieved via the isomerization and hydrolysis of SP6.

Chemistry Letters published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C3H6BrNaO3S, HPLC of Formula: 638-45-9.

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

Chen, Yuqing published the artcileSynthesis of Homoallylic Amines by Radical Allylation of Imines with Butadiene under Photoredox Catalysis, HPLC of Formula: 638-45-9, the publication is Angewandte Chemie, International Edition (2022), 61(29), e202204516, database is CAplus and MEDLINE.

A conceptually different radical-radical cross-coupling strategy for the synthesis of a homoallyl amines RCH₂CH=CHCH₂CH(NHR¹)(R²) (R = oxetan-3-yl, 3-methylbut-3-en-1-yl, 2-(tert-butoxy)-2-oxoethyl, etc.; R¹ = 4-fluorophenyl, 2,4,6-trimethylphenyl, naphthalen-2-yl, etc.; R² = thiophen-2-yl, 3,4-dimethoxyphenyl, 4-[methoxy(oxo)methyl]phenyl, etc.) between an α-amino alkyl radical and a transient allylic radical have been reported. This metal-free method provided a novel approach for the synthesis of homoallylic amines (>80 examples) from readily available materials with excellent regioselectivity and exceptional broad functional group compatibility.

Angewandte Chemie, International Edition published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C6H13I, HPLC of Formula: 638-45-9.

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

Lazaro-Milla, Carlos published the artcileMetal-Free C-C/C-N/C-C Bond Formation Cascade for the Synthesis of (Trifluoromethyl)sulfonylated Cyclopenta[b]indolines, Formula: C7H8INO, the publication is Organic Letters (2021), 23(8), 2921-2926, database is CAplus and MEDLINE.

A bis(triflyl)ethylation [triflyl = (trifluoromethyl)sulfonyl] inserted into a sequential cyclization cascade resulted in the direct formation of gem-bis(triflyl)ated cyclopenta[b]indolines from anilide-derived allenols and alkenols. This catalyst- and irradiation-free sequence facilitated the efficient preparation of functionalized tricyclic indoline cores bearing two contiguous stereocenters. The formed cyclopenta[b]indolines was easily transformed into a wide variety of triflylated indolines, including the tetracycle ring system found in polyveoline.

Organic Letters published new progress about 53279-83-7. 53279-83-7 belongs to iodides-buliding-blocks, auxiliary class Iodide,Amine,Benzene,Alcohol, name is (2-Amino-5-iodophenyl)methanol, and the molecular formula is C7H8INO, Formula: C7H8INO.

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

Tian, Zhenhao published the artcile“Domain Directional Optimization” strategy for the development of UGT1A1-activated fluorescent probe and the application in living systems, Application In Synthesis of 638-45-9, the publication is Sensors and Actuators, B: Chemical (2022), 132342, database is CAplus.

Activity-based fluorescent probes have emerged as the powerful tool for directly monitoring enzyme activity in living systems. Whereas, constructing high isoform-specific fluorescent probes for a target isoenzyme with multiple subtypes is still facing challenge. UGT1A1, as an isoform of UGTs, is a clear target for neonatal jaundice, irinotecan-induced toxicity, and fatal Crigler-Najjar syndrome type I. Herein, a “Domain Directional Optimization” strategy was proposed based on the systematic computational chem. and synchronously exptl. verification. Finally, an isoform-specific “switch-on” fluorescent probe (BUHE) was developed for UGT1A1 based on the boron-dipyrromethene (BODIPY) skeleton. BUHE exhibited the high selectivity and sensitivity toward UGT1A1 and the catalytic progress followed typical Michaelis-Menten kinetic. Moreover, BUHE had a good biocompatibility and chem. stability which was successfully applied to the activity evaluation and in situ imaging of UGT1A1 in complicated bio-systems including living cells, tissue slices and whole organs. In summary, the “Domain Directional Optimization” strategy could serve as a powerful method for developing the isoform-specific fluorescent probe.

Sensors and Actuators, B: Chemical published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C4H6O3, Application In Synthesis of 638-45-9.

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

Yamaga, Hiroaki published the artcileAmino acid derivative reactivity assay-organic solvent reaction system: A novel alternative test for skin sensitization capable of assessing highly hydrophobic substances, COA of Formula: C6H13I, the publication is Journal of Applied Toxicology (2021), 41(10), 1634-1648, database is CAplus and MEDLINE.

The amino acid derivative reactivity assay (ADRA) is an in chemico alternative to animal testing that focuses on protein binding. The ADRA is a skin sensitization test that solves problems associated with the direct peptide reactivity assay. However, when utilizing the ADRA to evaluate highly hydrophobic substances with octanol/water partition coefficients (logKow) of >6, the test substances may not dissolve in the reaction solution, which can prevent the accurate assessment of skin sensitization. Therefore, we developed the ADRA-organic solvent (ADRA-OS) reaction system, which is a novel skin sensitization test that enables the assessment of highly hydrophobic substances with a logKow of >6. We discovered that the organic solvent ratio, the triethylamine concentration, and the EDTA disodium salt dihydrate concentration participate in reactions with the nucleophile N-(2-(1-naphthyl)acetyl)-L-cysteine (NAC) and sensitizers that are used in ADRA and in stabilizing NAC. Thus, we determined the optimal reaction composition of the ADRA-OS according to L₉ (3³) orthogonal array experiments Using this test, we assessed 14 types of highly hydrophobic substances. When we compared the results with ADRA, we found that ADRA-OS reaction system has high solubility for highly hydrophobic substances and that it has a high predictive capacity (sensitivity: 63%, specificity: 100%, accuracy: 79%). The implication of the results is that the novel ADRA-OS reaction system should provide a useful method for assessing the skin sensitization of highly hydrophobic substances with a logKow of >6.

Journal of Applied Toxicology published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C10H14O2, COA of Formula: C6H13I.

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

Sabbatini, Paola published the artcileDesign, Synthesis, and in Vitro Pharmacology of New Radiolabeled γ-Hydroxybutyric Acid Analogues Including Photolabile Analogues with Irreversible Binding to the High-Affinity γ-Hydroxybutyric Acid Binding Sites, Quality Control of 53279-83-7, the publication is Journal of Medicinal Chemistry (2010), 53(17), 6506-6510, database is CAplus and MEDLINE.

γ-Hydroxybutyric acid (GHB) is a psychotropic compound endogenous to the brain. Despite its potential physiol. significance, the complete mol. mechanisms of action remain unexplained. To facilitate the isolation and identification of the high-affinity GHB binding site, we herein report the design and synthesis of the first ¹²⁵I-labeled radioligands in the field, one of which contains a photoaffinity label which enables it to bind irreversibly to the high-affinity GHB binding sites.

Journal of Medicinal Chemistry published new progress about 53279-83-7. 53279-83-7 belongs to iodides-buliding-blocks, auxiliary class Iodide,Amine,Benzene,Alcohol, name is (2-Amino-5-iodophenyl)methanol, and the molecular formula is C7H8INO, Quality Control of 53279-83-7.

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