Month: December 2022

Lorenc, Chris published the artcileAcid mediated deprotection of N-isopropyl tertiary amides, Application of 2-Isopropylanisole, the publication is Tetrahedron Letters (2015), 56(10), 1280-1282, database is CAplus.

Tertiary amides containing an N-iso-Pr group were selectively deprotected by heating in methanesulfonic acid. The N-iso-Pr group was removed selectively in the presence of other groups on the amide nitrogen such as Me, primary alkyl, or aryl. The putative iso-Pr cation was trapped by Friedel-Crafts alkylation of anisole when the latter was included as a co-solvent.

Tetrahedron Letters 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 C10H14O, Application of 2-Isopropylanisole.

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

Lu, Zijie published the artcileElaboration of microporous CeO₂ thin layers having nanocrystallites network controlled by Pluronic P123: Impact of key experimental parameters, Related Products of ethers-buliding-blocks, the publication is Journal of Sol-Gel Science and Technology (2020), 94(1), 174-185, database is CAplus.

Thus, a compromise between the crystallization and the preservation of the porosity needs to be found. This loss of nanocrystallites organization is more drastic in the direction perpendicular to the surface and less pronounced along the surface. Finally, an increase of the thermal treatment temperature from 300 to 1000°C leads to the formation of fluorite-like dioxide material coupled with a loss of nanocrystallites organization and porosity due to the increase of the size of the crystallites. The results show that the organization of the nanoparticles is possible for a sol ageing time lower than 16 days and that the size of the mesophase within the thin layer increases with the relative humidity fixed during the film deposition. The impact of key exptl. parameters, i.e., the sol ageing, the relative humidity (RH), the thermal treatment, on the thin layer elaboration were investigated. Microporous ceria thin films having nanocrystallites network were synthesized by evaporation-induced self-assembly process, using P123 amphiphilic copolymer as structure-directing agent.

Journal of Sol-Gel Science and Technology published new progress about 1589-47-5. 1589-47-5 belongs to ethers-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Alcohol,Ether, name is 2-Methoxypropan-1-ol, and the molecular formula is C4H10O2, Related Products of ethers-buliding-blocks.

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

Park, Sei-Kyoung published the artcileInhibition of Aβ42 oligomerization in yeast by a PICALM ortholog and certain FDA approved drugs, HPLC of Formula: 637-58-1, the publication is Microbial Cell (2016), 3(2), 53-64, database is CAplus and MEDLINE.

The formation of small Aβ42 oligomers has been implicated as a toxic species in Alzheimer disease (AD). In strong support of this hypothesis we found that overexpression of Yap1802, the yeast ortholog of the human AD risk factor, phosphatidylinositol binding clathrin assembly protein (PICALM), reduced oligomerization of Aβ42 fused to a reporter in yeast. Thus we used the Aβ42-reporter system to identify drugs that could be developed into therapies that prevent or arrest AD. From a screen of 1,200 FDA approved drugs and drug-like small compounds we identified 7 drugs that reduce Aβ42 oligomerization in yeast: 3 antipsychotics (bromperidol, haloperidol and azaperone), 2 anesthetics (pramoxine HCl and dyclonine HCl), tamoxifen citrate, and minocycline HCl. Also, all 7 drugs caused Aβ42 to be less toxic to PC12 cells and to relieve toxicity of another yeast AD model in which Aβ42 aggregates targeted to the secretory pathway are toxic. Our results identify drugs that inhibit Aβ42 oligomers from forming in yeast. It remains to be determined if these drugs inhibit Aβ42 oligomerization in mammals and could be developed as a therapeutic treatment for AD.

Microbial Cell published new progress about 637-58-1. 637-58-1 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is 4-(3-(4-Butoxyphenoxy)propyl)morpholine hydrochloride, and the molecular formula is C17H28ClNO3, HPLC of Formula: 637-58-1.

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

Sakya, Subas M. published the artcileEfficient synthesis of 5-alkyl amino and thioether substituted pyrazoles, Synthetic Route of 52818-63-0, the publication is Tetrahedron Letters (2003), 44(41), 7629-7632, database is CAplus.

Nucleophilic substitution reactions of 1-(4-methylsulfonyl-2-pyridyl)-5-chloro pyrazoles with various substitutions at the 4 position with amine nucleophiles and thiols occur under mild conditions to provide the 5-alkylamino and thioether pyrazoles in high yields. Reaction products of 4-chloro-1-[5-(methylsulfonyl)-2-pyridinyl]-3-(trifluoromethyl)-1H-pyrazole-4-carboxaldehyde with piperazine derivatives, benzenethiol, 1H-imidazole, cyclohexanethiol, 2(1H)-pyridinethione, etc. were reported. A similar reaction of 4-chloro-1-[5-(methylsulfonyl)-2-pyridinyl]-3-(trifluoromethyl)-1H-pyrazole-4-carbonitrile, 4-chloro-1-[5-(methylsulfonyl)-2-pyridinyl]-3-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid Me ester and 4-chloro-1-[5-(methylsulfonyl)-2-pyridinyl]-3-(trifluoromethyl)-1H-pyrazole-4-carboxamide with amines was also reported.

Tetrahedron Letters 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, Synthetic Route of 52818-63-0.

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

Jazayeri, Ali published the artcileCrystal structure of the GLP-1 receptor bound to a peptide agonist, Synthetic Route of 77128-73-5, the publication is Nature (London, United Kingdom) (2017), 546(7657), 254-258, database is CAplus and MEDLINE.

Glucagon-like peptide 1 (GLP-1) regulates glucose homeostasis through the control of insulin release from the pancreas. GLP-1 peptide agonists are efficacious drugs for the treatment of diabetes. To gain insight into the mol. mechanism of action of GLP-1 peptides, here we report the crystal structure of the full-length GLP-1 receptor bound to a truncated peptide agonist. The peptide agonist retains an α-helical conformation as it sits deep within the receptor-binding pocket. The arrangement of the transmembrane helixes reveals hallmarks of an active conformation similar to that observed in class A receptors. Guided by this structural information, we design peptide agonists with potent in vivo activity in a mouse model of diabetes.

Nature (London, United Kingdom) 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, Synthetic Route of 77128-73-5.

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

Schmidtchen, Franz P. published the artcilePolyprenylpyridinols. Synthesis of piericidin analogs, Recommanded Product: 2-Methoxyacetamide, the publication is Journal of the American Chemical Society (1977), 99(21), 7014-19, database is CAplus and MEDLINE.

The piericidin A analogs I (n = 1, 2, 3, 9) and II were prepared for structure-activity studies on coenzyme Q inhibitors. To prepare the nucleus, 3-methoxyacetylamino-2-methylacrylonitrile was cyclized to a 4-amino-2-pyridone which Me₃O⁺ BF₄^– converted to the 4-amino-2,3-dimethoxypyridine. Bromination of the acylated amine formed the 6-bromo derivative in which the 4-amino group was then replaced by hydroxy and the latter blocked by conversion to its benzyl ether with a benzylisourea. Transmetalation now gave the 6-lithio compound which was coupled with various prenyl bromides, leading to introduction of all trans polyprenyl side chains. The final 4-pyridinols were formed on selective debenzylation with butyl mercaptide. All the polyprenylpyridinols inhibited coenzyme Q electron transport to some extent, with the farnesyl analog having the same activity as piericidin A.

Journal of the American Chemical Society 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 C3H7NO2, Recommanded Product: 2-Methoxyacetamide.

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

Brown, Herbert C. published the artcileB-2′-Isoprenyldiisopinocampheylborane: an efficient reagent for the chiral isoprenylation of aldehydes. A convenient route to both enantiomers of ipsenol and ipsdienol, Related Products of ethers-buliding-blocks, the publication is Tetrahedron Letters (1990), 31(4), 455-8, database is CAplus.

B-2′-Isoprenyldiisopinocampheylborane is prepared by metalation of isoprene with potassium 2,2,5,5-tetramethylpiperidide followed by sequential treatment with B-methoxydiisopinocampheylborane and boron trifluoride-etherate. Condensation of this reagent with aldehydes provides isoprenylated chiral alcs. This methodol. is utilized for an efficient one-pot synthesis of both enantiomers of the pheromones of the bark beetle Ips paraconfusus Lanier, ipsenol (I) and ipsdienol (II) in 96% ee and 65% isolated yield.

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, Related Products of ethers-buliding-blocks.

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

Brown, Gerbert C. published the artcileChiral synthesis via organoboranes. 26. An efficient synthesis of isoprenyl derivatives of borane. Valuable reagents for the isoprenylboration of aldehyde. A convenient route to both enantiomers of ipsenol and ipsdienol in high optical purity, COA of Formula: C21H37BO, the publication is Tetrahedron (1990), 46(13-14), 4463-72, database is CAplus.

Preparation of B-isoprenyldialkylboranes is achieved by adopting the Brandsma modification of the Schlosser procedure, namely metalation of isoprene with potassium 2,2,5,5-tetramethylpiperidide followed by sequential treatment with B-methoxydialkylborane and boron trifluoride-etherate. These reagents are used for the convenient isoprenylation of aldehydes. Reaction of isovaleraldehyde and β,β-dimethylacrolein with B-2′-isoprenyldiisopinocampheylborane (I) provides both ipsenol (II) and ipsdienol (III), resp. in 65% yields and 96% ee.

Tetrahedron 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, COA of Formula: C21H37BO.

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

Martinez-Asencio, Ana published the artcileN-Alkylation of poor nucleophilic amine and sulfonamide derivatives with alcohols by a hydrogen autotransfer process catalyzed by copper(II) acetate, HPLC of Formula: 52818-63-0, the publication is Tetrahedron Letters (2010), 51(2), 325-327, database is CAplus.

Copper(II) acetate is a versatile, cheap, and simple catalyst for the selective N-monoalkylation of amino derivatives with poor nucleophilic character, such as aromatic and heteroaromatic amines as well as sulfonamides, using in all cases primary alcs. as initial source of the electrophiles, through a hydrogen autotransfer process. In the case of sulfonamides, the monoalkylation process followed by a naphthalene-catalyzed reductive deprotection gives primary amines, which is an indirect alternative to the direct monoalkylation of ammonia.

Tetrahedron Letters 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, HPLC of Formula: 52818-63-0.

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

Martinez-Asencio, Ana published the artcileN-Alkylation of poor nucleophilic amines and derivatives with alcohols by a hydrogen autotransfer process catalyzed by copper(II) acetate: Scope and mechanistic considerations, COA of Formula: C13H14N2O, the publication is Tetrahedron (2011), 67(17), 3140-3149, database is CAplus.

Copper(II) acetate is a versatile, cheap and simple catalyst for the selective N-monoalkylation of amino derivatives with poor nucleophilic character, such as aromatic and heteroaromatic amines as well as carboxamides, phosphinamides, sulfonamides, and phosphazenes, using in all cases primary alcs. as initial source of the electrophiles, through a hydrogen autotransfer process. In the case of sulfonamides, the monoalkylation process followed by a naphthalene-catalyzed reductive deprotection gives primary amines, which is an indirect alternative to the direct monoalkylation of ammonia. A study of the reaction using deuterium labeled reagents was performed, indicating that the dehydrogenation and hydrogenation steps do not take place on the same copper-atom coordination sphere, with the condensation step occurring out of the dehydrogenating catalytic species.

Tetrahedron 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, COA of Formula: C13H14N2O.

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