Month: December 2022

Thomae, David published the artcileIdentification and in vivo evaluation of a fluorine-18 rolipram analogue, [¹⁸F]MNI-617, as a radioligand for PDE4 imaging in mammalian brain, SDS of cas: 17351-62-1, the publication is Journal of Labelled Compounds and Radiopharmaceuticals (2016), 59(5), 205-213, database is CAplus and MEDLINE.

Phosphodiesterase (PDE) 4 is the most prevalent PDE in the central nervous system (CNS) and catalyzes hydrolysis of intracellular cAMP, a secondary messenger. By therapeutic inhibition of PDE4, intracellular cAMP levels can be stabilized, and the symptoms of psychiatric and neurodegenerative disorders including depression, memory loss and Parkinson’s disease can be ameliorated. Radiotracers targeting PDE4 can be used to study PDE4 d. and function, and evaluate new PDE4 therapeutics, in vivo in a non-invasive way, as has been shown using the carbon-11 labeled PDE4 inhibitor R-(-)-rolipram. Herein we describe a small series of rolipram analogs that contain fluoro- or iodo-substituents that could be used as fluorine-18 PET or iodine-123 SPECT PDE4 radiotracers. This series was evaluated with an in vitro binding assay and a 4-(fluoromethyl) derivative of rolipram, MNI-617, was identified, with a five-fold increase in affinity for PDE4 (K_d = 0.26 nM) over R-(-)-rolipram (K_d = 1.6 nM). A deutero-analog d₂-[¹⁸F]MNI-617 was radiolabeled and produced in 23% yield with high (>5 Ci/¦Ìmol) specific activity and evaluated in non-human primate, where it rapidly entered the brain, with SUVs between 4 and 5, and with a distribution pattern consistent with that of PDE4.

Journal of Labelled Compounds and Radiopharmaceuticals published new progress about 17351-62-1. 17351-62-1 belongs to catalysis-chemistry, auxiliary class Salt,Amine, name is Tetrabutylammonium hydrogencarbonate, and the molecular formula is C16H24BF4Ir, SDS of cas: 17351-62-1.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Okuno, Masataka published the artcileProtease inhibitors suppress TGF-¦Â generation by hepatic stellate cells, Product Details of C17H19N3O7S, the publication is Journal of Hepatology (1998), 29(6), 1031-1032, database is CAplus and MEDLINE.

Transforming growth factor-¦Â is the major cytokine implicated in the pathogenesis of liver fibrosis and cirrhosis. The authors decided to examine which protease inhibitors would be effective in suppressing TGF-¦Â generation. The data suggest that these compounds might be beneficial for the therapy of the liver fibrosis. Tranexamic acid has been used episodically as a cytoprotective agent against liver damage.

Journal of Hepatology published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, Product Details of C17H19N3O7S.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Burmistrov, Vladimir published the artcileEffects of adamantane alterations on soluble epoxide hydrolase inhibition potency, physical properties and metabolic stability, Computed Properties of 14707-75-6, the publication is Bioorganic Chemistry (2018), 510-527, database is CAplus and MEDLINE.

Adamantyl groups are widely used in medicinal chem. However, metabolism limits their usage. Herein, the authors report the first systematic study of adamantyl ureas and diureas bearing substituents in bridgehead positions of adamantane and/or spacers between urea groups and adamantane group, and tested their effects on soluble epoxide hydrolase inhibitor potency and metabolic stability. Interestingly, the effect on activity against human and murine sEH varied in opposite ways with each new Me group introduced into the mol. Compounds with three Me substituents in adamantane were very poor inhibitors of murine sEH while still very potent against human sEH. In addition, diureas with terminal groups bigger than sEH catalytic tunnel diameter were still good inhibitors suggesting that the active site of sEH opens to capture the substrate or inhibitor mol. The introduction of one Me group leads to 4-fold increase in potency without noticeable loss of metabolic stability compared to the unsubstituted adamantane. However, introduction of two or three Me groups leads to 8-fold and 98-fold decrease in stability in human liver microsomes for the corresponding compounds

Bioorganic Chemistry published new progress about 14707-75-6. 14707-75-6 belongs to catalysis-chemistry, auxiliary class Triazinanes, name is 1,3,5-Triazaadamantan-7-amine, and the molecular formula is C7H14N4, Computed Properties of 14707-75-6.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Shimizu, Daiki published the artcileNucleophilic Aromatic Substitution Reactions of meso-Bromosubporphyrin: Synthesis of a Thiopyrane-Fused Subporphyrin, Product Details of C12H9N3O4, the publication is Chemistry – A European Journal (2014), 20(49), 16194-16202, database is CAplus and MEDLINE.

Meso-Bromosubporphyrin undergoes nucleophilic aromatic substitution (S_NAr) reactions with arylamines, diarylamines, phenols, EtOH, thiophenols, and n-butanethiol in the presence of suitable bases to provide the corresponding substitution products. The S_NAr reactions also proceed well with pyrrole, indole, and carbazole to provide substitution products in moderate to good yields. Finally, the S_NAr reaction with 2-bromothiophenol and subsequent intramol. peripheral arylation reaction affords a thiopyrane-fused subporphyrin.

Chemistry – A European Journal published new progress about 1821-27-8. 1821-27-8 belongs to catalysis-chemistry, auxiliary class Nitro Compound,Amine,Benzene, name is Bis(4-nitrophenyl)amine, and the molecular formula is C30H32ClN7O2, Product Details of C12H9N3O4.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Sergeev, Maxim E. published the artcileTitania-Catalyzed Radiofluorination of Tosylated Precursors in Highly Aqueous Medium, Product Details of C17H37NO3, the publication is Journal of the American Chemical Society (2015), 137(17), 5686-5694, database is CAplus and MEDLINE.

Nucleophilic radiofluorination is an efficient synthetic route to many positron-emission tomog. (PET) probes, but removal of water to activate the cyclotron-produced [¹⁸F]fluoride has to be performed prior to reaction, which significantly increases overall radiolabeling time and causes radioactivity loss. In this report, we demonstrate the possibility of ¹⁸F-radiofluorination in highly aqueous medium. The method utilizes titania nanoparticles, 1:1 (volume/volume) acetonitrile-thexyl alc. solvent mixture, and tetra-n-butylammonium bicarbonate as a phase-transfer agent. Efficient radiolabeling is directly performed with aqueous [¹⁸F]fluoride without the need for a drying/azeotroping step to significantly reduce radiosynthesis time. High radiochem. purity of the target compound is also achieved. The substrate scope of the synthetic strategy is demonstrated with a range of aromatic, aliphatic, and cycloaliphatic tosylated precursors.

Journal of the American Chemical Society published new progress about 17351-62-1. 17351-62-1 belongs to catalysis-chemistry, auxiliary class Salt,Amine, name is Tetrabutylammonium hydrogencarbonate, and the molecular formula is C10H16O2, Product Details of C17H37NO3.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Tristany, Mar published the artcileSelf-assembled platinum nanoparticles into heavily fluorinated templates: Reactive gas effect on the morphology, Application of 3,3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,10-Heptadecafluorodecan-1-amine, the publication is New Journal of Chemistry (2009), 33(7), 1529-1534, database is CAplus.

The synthesis of platinum(0) nanoparticles by decomposition of Pt₂(dba)₃ under a dihydrogen or CO atm. and in the presence of heavily fluorinated stabilizers is described. Several techniques were used for the characterization of the obtained nanomaterials (TEM, HREM, WAXS and SEM-FEG) that organize into spherical or elongated superstructures made of small individual nanoparticles (?2.5 nm).

New Journal of Chemistry published new progress about 30670-30-5. 30670-30-5 belongs to catalysis-chemistry, auxiliary class Polyfluoroalkanes, name is 3,3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,10-Heptadecafluorodecan-1-amine, and the molecular formula is C16H12O, Application of 3,3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,10-Heptadecafluorodecan-1-amine.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Legnani, Luca published the artcileDirect Catalytic Synthesis of Unprotected 2-Amino-1-Phenylethanols from Alkenes by Using Iron(II) Phthalocyanine, Recommanded Product: O-Pivaloylhydroxylamine trifluoromethanesulfonate, the publication is Angewandte Chemie, International Edition (2016), 55(6), 2248-2251, database is CAplus and MEDLINE.

Aryl-substituted amino alcs. are privileged scaffolds in medicinal chem. and natural products. Herein, we report that an exceptionally simple and inexpensive Fe^II complex efficiently catalyzes the direct transformation of simple alkenes into unprotected amino alcs. in good yield and perfect regioselectivity. This new catalytic method was applied in the expedient synthesis of bioactive mols. and could be extended to aminoetherification.

Angewandte Chemie, International Edition published new progress about 1293990-73-4. 1293990-73-4 belongs to catalysis-chemistry, auxiliary class Aliphatic Chain, name is O-Pivaloylhydroxylamine trifluoromethanesulfonate, and the molecular formula is C6H12F3NO5S, Recommanded Product: O-Pivaloylhydroxylamine trifluoromethanesulfonate.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Won Kang, Hye published the artcileESR and NMR probes of counter-ion effects in perfluorosulfonate ionomer membranes, COA of Formula: C19H42F6NP, the publication is Journal of Membrane Science (1998), 148(2), 173-184, database is CAplus.

The properties of Nafion membranes, modified by exchange with tetraalkylammonium cations and equilibrated in methanol, were investigated using ESR spin probe techniques and ¹⁴N NMR spectroscopy. TEMPO and TEMPOL nitroxide radicals are shown to act as probes of the methanol solvent phase of the membranes. The mobility of the probe radicals is restricted, the correlation times for rotational diffusion being reduced by an order of magnitude within the ionomer environment compared to free methanol solution The larger tetraalkylammonium cations result in higher levels of swelling in methanol and a greater degree of nitroxide mobility. The temperature dependent ESR spectra show a gradual transition from freely diffusing to rigidly immobilized radicals as the temperature is lowered. The motion is completely frozen out at about 190 K, before the f.p. of methanol is reached. ¹⁴N NMR spectroscopy of the tetraalkylammonium counter-ions is also reported. The NMR signals for all cations remain quite sharp and well resolved in methanol-equilibrated Nafion. The corresponding ¹⁴N spin lattice relaxation times, T₁, were reduced by one order of magnitude compared to methanol solution The long-chain surfactant cations showed the least reduction in T₁ on incorporation into the membrane, consistent with retention of significant rotational mobility. These results are interpreted in terms of a much weaker ion clustering in the organically modified membranes than is found in strongly hydrated Nafion membranes.

Journal of Membrane Science published new progress about 101079-29-2. 101079-29-2 belongs to catalysis-chemistry, auxiliary class Surfactants, name is N-hexadecyltrimethylammoniumhexafluorophosphate, and the molecular formula is C23H43NP2, COA of Formula: C19H42F6NP.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Ramos Chagas, Gabriela published the artcileSuperhydrophobic and fluorescent properties of fluorinated polypyrene surfaces using various polar linkers prepared via electropolymerization, Application of 3,3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,10-Heptadecafluorodecan-1-amine, the publication is Reactive & Functional Polymers (2019), 65-76, database is CAplus.

Superhydrophobic and fluorescent polypyrene surfaces were synthesized by an electropolymerization process. Six different linkers (ester, thioester, amide, carbamate, thiocarbamate and urea) are used to introduce fluorinated chains (lengths of 4, 6 and 8 carbons) onto pyrene moiety. The electropolymerized surfaces were analyzed by their morphol., surface chem., wettability and fluorescence. The linkers and the length of the fluorinated chain influence on both surface chem. and morphol. confirmed by XPS and SEM anal., resp. Superhydrophobic surfaces were obtained for ester, thioester, carbamate and thiocarbamate series while high hydrophobic surfaces for amide and urea series. Here, we show the possibility to control the surface hydrophobicity, oleophobicity and liquid adhesion with both the linker and the fluorinated chain length. For example, N-H groups seem to induce a decrease in the static contact angle (¦È_w) and in the surface structuration due to their polarity generating smoother surfaces (as for amide and urea series) and yielding to a red-shift in the emission spectra (showed for amide, carbamate, thiocarbamate and urea). The emission of all the polypyrene films is red-shifted compared to the pyrene monomers (excimer emission) and in the green region independently of the side chain. Here, we show that the nature of the heteroatom that connects the pyrene moiety to the fluorinated chain also does great impact on the surface morphol., wetting and fluorescence properties.

Reactive & Functional Polymers published new progress about 30670-30-5. 30670-30-5 belongs to catalysis-chemistry, auxiliary class Polyfluoroalkanes, name is 3,3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,10-Heptadecafluorodecan-1-amine, and the molecular formula is C10H6F17N, Application of 3,3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,10-Heptadecafluorodecan-1-amine.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Dilworth, Jonathan R. published the artcileRhodium and iridium complexes with thiolate and tertiary phosphine ligands. The synthesis and structures of trans-[Ir(SC₆H₃Cl₂-2,6)(CO)(PPh₃)₂], [Rh₂(¦Ì-SC₆H₃Prⁱ₃-2,4,6)₂(CO)₂(PPh₃)₂], [Rh₂H₂(¦Ì-SC₆H₄PPh₂-2)₂(CO)₂(PPh₃)₂][BF₄]₂, and [Rh₂I₆(MeSC₆H₄PPh₂-2)₂], Related Products of catalysis-chemistry, the publication is Dalton (2000), 3007-3015, database is CAplus.

Reaction of [MF(CO)(PPh₃)₂] (M = Rh or Ir) with bulky aromatic thiols ArSH gave binuclear [M₂(¦Ì-SAr)₂(CO)₂(PPh₃)₂] (M = Rh, SAr = SC₆H₂Prⁱ₃-2,4,6 or SC₆H₃Me₂-2,6) and mononuclear [M(SAr)(CO)(PPh₃)₂] (M = Rh or Ir, SAr = SC₆H₃Cl₂-2,6 or SC₆H₄SiPh₃-2; M = Ir, SAr = SC₆H₂Prⁱ₃-2,4,6 or SC₆H₃Me₂-2,6). The crystal structure of [Rh₂(¦Ì-SC₆H₃Prⁱ₃-2,4,6)₂(CO)₂(PPh₃)₂] showed a binuclear thiolate bridged core while that of [Ir(SC₆H₃Cl₂-2,6)(CO)(PPh₃)₂] revealed a conventional square planar geometry with trans PPh₃ ligands. Three Rh complexes are efficient catalysts for the hydroformylation of hept-1-ene under mild conditions with good selectivity for linear aldehyde for SAr = SC₆H₄SiPh₃-2. Reaction of [MF(CO)(PPh₃)₂] with phosphinothiolate proligands PSH gave monomeric [M(PS)(CO)(PPh₃)₂] (M = Rh or Ir; PS = SC₆H₄PPh₂-2 or S(CH₂)₃PPh₂; M = Rh, PS = SCH₂CH₂PPh₂ or SCHMeCH₂PPh₂). [Rh(SC₆H₄PPh₂-2)(CO)(PPh₃)] reacted reversibly with protons (HBF₄) to give the dimeric dication [Rh₂(¦Ì-SC₆H₄PPh₂-2)₂(CO)₂(PPh₃)₂]²⁺, shown by a crystal structure be a thiolate bridged dimer with an Rh-Rh bond and pseudo-octahedral geometry about each Rh^III. Electrophilic attack by [Me₃O][BF₄] on [Rh(SC₆H₄PPh₂-2)(CO)(PPh₃)] occurred at S to give [Rh(MeSC₆H₄PPh₂-2)(CO)(PPh₃)]⁺ and excess of MeI gave [Rh₂I₆(MeSC₆H₄PPh₂-2)₂], with octahedral Rh^III linked by a double iodide bridge. Attack at S also occurred in [Rh(SC₆H₄PPh₂-2)(CO)(PPh₃)] with I(CH₂)₃I and ICH₂CO₂H to give [Rh(2-Ph₂PC₆H₄SCH₂CH₂CH₂)(CO)(PPh₃)] and [RhI₂(2-Ph₂PC₆H₄SCH₂CO₂)(PPh₃)], resp. [RhI₃(CO)(PPh₃)₂] was a byproduct and shown by a crystal structure to have a pseudo-octahedral structure with trans-PPh₃ ligands.

Dalton published new progress about 22693-41-0. 22693-41-0 belongs to catalysis-chemistry, auxiliary class Other Functionalization Reagent, name is 2,4,6-Triisopropylbenzenethiol, and the molecular formula is C15H24S, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia