Month: December 2022

Liu, Bin published the artcileIonic liquid/boronic acid system enabled deuteration with D₂O, COA of Formula: C11H10O, the publication is Tetrahedron Letters (2022), 153968, database is CAplus.

The development of transition-metal free systems for multi-sites deuteration is important for the preparation of deuterium-labeled drugs and intermediates e.g, d-agomelatine. The ionic liquid [bmim]PF₆, which was able to promote highly efficient deuterodeborylation of boronic acids RB(OH)₂ [R = thianthren-1-yl, 1-benzothiophen-2-yl, 4-formyl-2-methoxyphenyl, etc.] with D₂O was reported. The ionic liquid/boronic acid system was successfully applied to the selective H/D exchange at various sp²/sp³ C-H positions. Moreover, unusual nucleophilic behaviors of nitrogen-containing heteroaromatics in ionic liquid were observed

Tetrahedron Letters published new progress about 93-04-9. 93-04-9 belongs to ethers-buliding-blocks, auxiliary class Naphthalene,Ether, name is 2-Methoxynaphthalene, and the molecular formula is C11H10O, COA of Formula: C11H10O.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Ramalho, Suelem D. published the artcileSynthesis, racemic X-ray crystallographic, and permeability studies of bioactive orbitides from Jatropha species, HPLC of Formula: 77128-73-5, the publication is Journal of Natural Products (2018), 81(11), 2436-2445, database is CAplus and MEDLINE.

Orbitides are small cyclic peptides with a diverse range of therapeutic bioactivities. They are produced by many plant species, including those of the Jatropha genus. Here, the objective was to provide new structural information on orbitides to complement the growing knowledge base on orbitide sequences and activities by focusing on three Jatropha orbitides: ribifolin, pohlianin C, and jatrophidin. To determine three-dimensional structures, racemic crystallog., an emerging structural technique that enables rapid crystallization of biomols. by combining equal amounts of the two enantiomers, was used. The high-resolution structure of ribifolin (0.99 Å) was elucidated from its racemate and showed it was identical to the structure crystallized from its L-enantiomer only (1.35 Å). Racemic crystallog. was also used to elucidate high-resolution structures of pohlianin C (1.20 Å) and jatrophidin (1.03 Å), for which there was difficulty forming crystals without using racemic mixtures The structures were used to interpret membrane permeability data in PAMPA and a Caco-2 cell assay, showing they had poor permeability. Overall, the results show racemic crystallog. can be used to obtain high-resolution structures of orbitides and is useful when enantiopure samples are difficult to crystallize or solution structures from NMR are of low resolution

Journal of Natural Products published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C25H23NO4, HPLC of Formula: 77128-73-5.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Paterson, Ian published the artcileStudies in marine macrolide synthesis: synthesis of a C₁₆-C₂₈ subunit of spongistatin 1 (altohyrtin A) incorporating the CD-spiroacetal moiety, Formula: C21H37BO, the publication is Tetrahedron Letters (1997), 38(51), 8911-8914, database is CAplus.

The C₁₆-C₂₈ ketone I, containing the CD-spiroacetal of spongistatin 1, was prepared in 17 steps from the aldehyde Me₃CSiMe₂OCH₂CH₂CHO. Both thermodn. and kinetic conditions were explored for controlling the CD-acetal configuration.

Tetrahedron Letters published new progress about 99438-28-5. 99438-28-5 belongs to ethers-buliding-blocks, auxiliary class Chiral,Aliphatic cyclic hydrocarbon, name is (+)-B-Methoxydiisopinocampheylborane, and the molecular formula is C21H37BO, Formula: C21H37BO.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Walker, James B. published the artcileInhibition of sulfhydryl enzymes by 1,1′-dithiodiformamidine, Name: Formamidine disulfide dihydrochloride, the publication is Archives of Biochemistry and Biophysics (1960), 86(No. 1), 80-4, database is CAplus and MEDLINE.

Based upon the reaction of SH groups with 1,1′-dithiodiformamidine (I), it is shown that the enzymes papain, urease, and arginineglycine transamidinase contain such groups. A mechanism for this reaction of I is proposed.

Archives of Biochemistry and Biophysics published new progress about 14807-75-1. 14807-75-1 belongs to ethers-buliding-blocks, auxiliary class Salt,Thiourea,Amine,Aliphatic hydrocarbon chain, name is Formamidine disulfide dihydrochloride, and the molecular formula is C9H6N2O2, Name: Formamidine disulfide dihydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Yokoyama, Naokata published the artcileSynthesis and Structure-Activity Relationships of Oxamic Acid and Acetic Acid Derivatives Related to L-Thyronine, Quality Control of 2944-47-0, the publication is Journal of Medicinal Chemistry (1995), 38(4), 695-707, database is CAplus and MEDLINE.

Aryloxamic acids I (R = NHCOCO₂H, R¹ = Br, Me) and II, (arylamino)acetic acids I (R = NHCHRCO₂H, R¹ = Cl, Me, iodo, R² = Gly-OH, Ala-OH, Phe-OH), arylpropionic acids I (R = CH₂CH₂CO₂H, R¹ = Br, Me), arylthioacetic acids I (R = SCH₂CO₂H, R¹ = Br, Me), and (aryloxy)acetic acid I (R = OCH₂CO₂H, R¹ = Br), related to L-triiodothyronine (L-T₃) were prepared and tested in vitro for binding to the rat liver nuclear L-T₃ receptor and the rat membrane L-T₃ receptor. The structure-activity relationships for the prepared compounds are described, with several I and II showing excellent potency to the nuclear receptor and significantly lower binding affinity to the membrane receptor (IC₅₀ > 5 μM). Some of these compounds, especially in the oxamic acid series I (R = NHCOCO₂H) and II, showed an unprecedented potency for methyl-substituted derivatives such as I (R = NHCOCO₂H, R¹ = Me) and (±)-II. I (R = NHCOCO₂H, R¹ = Me) and (±)-II showed good lipid lowering effects in rats with ED₅₀ = 20 and 5 μg/kg po, resp., and a lack of cardiac side effects in rats at doses as high as 10 and 25 mg/kg po, resp.

Journal of Medicinal Chemistry published new progress about 2944-47-0. 2944-47-0 belongs to ethers-buliding-blocks, auxiliary class Benzene,Ether, name is 2-Isopropylanisole, and the molecular formula is C6H12O2, Quality Control of 2944-47-0.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Bolzan, A. E. published the artcileElectrochemical response of thiourea and formamidine disulphide on polycrystalline platinum in aqueous 0.5 M sulphuric acid, Application of Formamidine disulfide dihydrochloride, the publication is Journal of Electroanalytical Chemistry (1999), 475(2), 181-189, database is CAplus.

The electrochem. response of both thiourea and formamidine disulfide dissolved in aqueous 0.5M sulfuric acid on polycrystalline platinum electrodes was studied at 298 K, using voltammetry and rotating ring-disk electrode techniques. The electrooxidation of thiourea on platinum involves two stages occurring in different potential windows. The 1st thiourea electrooxidation stage for E<0.7 V (vs. SCE), yielding soluble formamidine disulfide as the main product, behaves as an electrochem. process under intermediate kinetics. Kinetic parameters for the electrooxidation of thiourea are estimated The voltammetric electroreduction of formamidine disulfide dihydrochloride to thiourea is inhibited gradually by the adsorption of byproducts from the electrochem. reactions. The 2nd thiourea electrooxidation stage for E 0.7 V involves the oxidation of thiourea and adsorbed residues competing with the oxide monolayer formation on platinum.

Journal of Electroanalytical Chemistry published new progress about 14807-75-1. 14807-75-1 belongs to ethers-buliding-blocks, auxiliary class Salt,Thiourea,Amine,Aliphatic hydrocarbon chain, name is Formamidine disulfide dihydrochloride, and the molecular formula is C2H8Cl2N4S2, Application of Formamidine disulfide dihydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Tamura, Masazumi published the artcileEfficient and Substrate-Specific Hydration of Nitriles to Amides in Water by Using a CeO₂ Catalyst, SDS of cas: 16332-06-2, the publication is Chemistry – A European Journal (2011), 17(41), 11428-11431, S11428/1-S11428/6, database is CAplus and MEDLINE.

Cerium dioxide (CeO₂) is an effective heterogeneous catalyst for the hydration of nitriles that have a heteroatom (N or O) adjacent to the α carbon of the CN group. The substrate specificity is derived from an enormous difference of frequency factor. For the hydration of pyrazinecarbonitrile to pyrazinecarboxamide in water, CeO₂ shows higher activity than the state-of-the-art catalysts including enzymes. A Michaelis-Menten-type mechanism is proposed, which involves (1) H₂O dissociation on CeO₂, (2) adsorption of the nitrile on CeO₂, and (3) nucleophilic attack of a hydroxyl species to the adsorbed nitrile.

Chemistry – A European Journal published new progress about 16332-06-2. 16332-06-2 belongs to ethers-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Amide,Ether, name is 2-Methoxyacetamide, and the molecular formula is C4H6O3, SDS of cas: 16332-06-2.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Oguchi, Minoru published the artcileMolecular Design, Synthesis, and Hypoglycemic Activity of a Series of Thiazolidine-2,4-diones, Safety of 6-Methoxy-N2-methylpyridine-2,3-diamine, the publication is Journal of Medicinal Chemistry (2000), 43(16), 3052-3066, database is CAplus and MEDLINE.

A series of imidazopyridine thiazolidine-2,4-diones were designed and synthesized from their corresponding pyridines. These compounds represent conformationally restricted analogs of the novel hypoglycemic compound rosiglitazone. The series was evaluated for its effect on insulin-induced 3T3-L1 adipocyte differentiation in vitro and its hypoglycemic activity in the genetically diabetic KK mouse in vivo. The structure-activity relationships are discussed. On the basis of the in vivo potency, 5-[4-(5-methoxy-3-methyl-3H-imidazo[4,5-b]pyridin-2-ylmethoxy)benzyl]thiazolidine-2,4-dione was selected as the candidate for further studies in a clin. setting.

Journal of Medicinal Chemistry published new progress about 90817-34-8. 90817-34-8 belongs to ethers-buliding-blocks, auxiliary class Pyridine,Amine,Ether, name is 6-Methoxy-N2-methylpyridine-2,3-diamine, and the molecular formula is C7H11N3O, Safety of 6-Methoxy-N2-methylpyridine-2,3-diamine.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Lemmens, Vincent published the artcileRu-Bipyridine Entrapped in the Supercages of EMC-1 Faujasite as Catalyst for the Trifluoromethylation of Arenes, Application In Synthesis of 91-16-7, the publication is ACS Applied Materials & Interfaces (2022), 14(1), 971-977, database is CAplus and MEDLINE.

Trifluoromethyl (CF₃) groups are versatile structural motifs especially in the field of agrochems. and pharmaceuticals. However, current trifluoromethylation reactions are generally associated with stoichiometric amounts of transition metals/metal oxidants, homogeneous catalysts, high temperatures, and expensive trifluoromethylating agents. In this work, the homogeneous photocatalyst Ru(bipy)₃²⁺ is entrapped in the pores of a faujasite support (EMC-1) via a “ship-in-a-bottle” strategy. The formation of the coordination compound was confirmed by Fourier transform IR (FTIR), UV-Vis spectroscopy, and X-ray absorption spectroscopy (XAS). Due to its high stability toward acidified environments, this single-site heterogeneous catalyst is suitable for the trifluoromethylation of synthetically interesting (hetero)arenes under visible-light irradiation at room temperature Furthermore, the heterogeneous catalyst could efficiently be reused for at least three times with minimal catalyst leaching/deactivation.

ACS Applied Materials & Interfaces published new progress about 91-16-7. 91-16-7 belongs to ethers-buliding-blocks, auxiliary class Benzene,Ether,Inhibitor,Inhibitor,Inhibitor, name is 1,2-Dimethoxybenzene, and the molecular formula is C8H10O2, Application In Synthesis of 91-16-7.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Chatenoud, Lucienne published the artcilePolyclonal and monoclonal antibodies directed against SK & F 94461, a specific H₁ histamine receptor ligand, Recommanded Product: N-(4-Methoxybenzyl)pyridin-2-amine, the publication is Molecular Pharmacology (1988), 34(2), 136-44, database is CAplus and MEDLINE.

SK & F 944618 an aminopentyl analog of mepyramine, is a recently described H, receptor antagonist. At variance with the other available H₁ receptor ligands, SK & F 94461 offers the possibility of coupling to a protein carrier to render the mol. immunogenic. SK & F 94461 coupled to succinylated bovine serum albumin was used as an immunogen to raise polyclonal antibodies in rabbits and BALB/c mice. In parallel, spleen cells from immunized mice were used to produce hybridomas by somatic cell fusion. Thus, 6 different murine monoclonal antibodies sharing anti-SK & F 94461 specificity were selected for further detailed characterization of their binding properties. Pharmacol. studies of competitive inhibition by using a set of 11 histaminergic agents allowed anal. of the fine specificity of anti-SK & F 94461 antibodies. Both polyclonal and monoclonal anti-SK & F 94461 antibodies showed very high affinity for the immunizing mol. (i.e., K_a values for monoclonal antibodies 8 and 12 were, resp., 3 × 10¹⁰ and 1.4 × 10¹⁰ M^-1). Both types of antibodies bound with high affinity (IC₅₀ ranging from 10^-10-10^-12 M) to mepyramine, which has a chem. structure closely resembling that of SK & F 94461. Moreover, these antibodies displayed clear-cut stereoselectivity inasmuch as they bound the d-configuration of chlorpheniramine with higher affinity than the l-form. Thus, all 6 monoclonal antibodies showed IC₅₀ values 1-6 log units lower for d– than for l-chlorpheniramine. For some monoclonal antibodies, spectroscopic and fluorescence spectra studies showed that their different binding capacities correlated with their optical properties. Similarly, polyclonal anti-SK & F 94461 antibodies showed a 500-fold lower affinity for l– than for d-chlorpheniramine. All these results indicate that the polyclonal and the majority of monoclonal anti-SK & F 94461 antibodies recognized with high-affinity structural configurations known to be important for the pharmacol. activity of H₁ ligands, namely the presence of the dimethylaminoethyl side chain and, with stereochem. selectivity, the d-configuration of chlorpheniramine. These data extend for the 1st time to an H₁ histamine receptor ligand results reported in other hormone systems.

Molecular Pharmacology published new progress about 52818-63-0. 52818-63-0 belongs to ethers-buliding-blocks, auxiliary class Pyridine,Amine,Benzene,Ether, name is N-(4-Methoxybenzyl)pyridin-2-amine, and the molecular formula is C13H14N2O, Recommanded Product: N-(4-Methoxybenzyl)pyridin-2-amine.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem