Rachel A Weintraub,Wei He,Xiang Wang
Rachel A Weintraub
Using an isoindole umpolung strategy, a one-pot synthesis of polycyclic isoindolines was accomplished. In this reaction, the in situ-generated nucleophilic isoindoles were converted to electrophilic isoindoliums via protonation, which under...
Synthesis of a boron-containing amidoxime reagent and its application to synthesize functionalized oxadiazole and quinazolinone derivatives [0.03%]
含硼胺氧亚胺试剂的合成及其在功能性噁二唑和喹唑啉酮衍生物中的应用
Bhaskar C Das,Nitesh K Nandwana,Devi P Ojha et al.
Bhaskar C Das et al.
Herein, we report the design, synthesis and application of a borylated amidoxime reagent for the direct synthesis of functionalized oxadiazole and quinazolinone derivatives. This reagent exhibits broad synthetic utility to obtain a variety ...
Synthesis of α-substituted 2-(1 H-1,2,4-triazol-3-yl)acetates and 5-amino-2,4-dihydro-3 H-pyrazol-3-ones via the Pinner strategy [0.03%]
通过Pinner策略合成α-取代的2-(1H-1,2,4-三唑-3-基)乙酸酯和5-氨基-2,4-二氢-3H-吡唑-3-酮
Dmytro M Khomenko,Roman O Doroshchuk,Hanna V Ivanova et al.
Dmytro M Khomenko et al.
A series of 2-(1H-1,2,4-triazol-3-yl)acetates, as well as 4-mono- and 4,4-disubstituted 5-amino-2,4-dihydro-3H-pyrazol-3-ones (including spirocyclic derivatives) have been synthesized using the Pinner reaction strategy. α-Mono- and α,α-d...
Lindsey O Calabretta,Vienna M Thomas,Ronald T Raines
Lindsey O Calabretta
Octanol-water partitioning experiments in the presence of carboxylate-, phosphate-, and sulfate-containing anionic lipids revealed that Ac-Cav-NH2 (where Cav refers to δ-oxa-arginine) partitions less into octanol than does Ac-Arg-NH2, sugg...
Amy C Jackson,James T Olsen,Sasha Sundstrom et al.
Amy C Jackson et al.
A ring expansion of tetramic acids (pyrrolidine-2,4-diones) to N-oxy-2,5-diketopiperazines (DKPs) is described. This method allows for the facile and late-stage construction of the hydroxamic acid moiety and can thereby serve as a general m...
Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs [0.03%]
合成并评估GS-441524的同位素类似物对抗SARS-CoV-2的活性
Wei Zheng,Tianwen Hu,Yumin Zhang et al.
Wei Zheng et al.
The COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is continuing to spread around the world. GS-441524 is the parent nucleoside of remdesivir which is the first drug approved for the treatment of COVID-19, a...
Amber M Kelley,Joshua A Frost,Tylisha M Baber et al.
Amber M Kelley et al.
Nitriles are important organic functional groups, allowing for installation of nitrogen in organic synthesis. The Pinner reaction transforms nitriles into esters via the imidate group, but in general has previously necessitated harsh acid c...
Regioselective alkylation of 2,4-dihydroxybenzyaldehydes and 2,4-dihydroxyacetophenones [0.03%]
2,4-二羟基苯甲醛和2,4-二羟基乙酰苯酮的区域选择性烷基化反应
Aziza Frank,Negar Hamidi,Fengtian Xue
Aziza Frank
We report a cesium bicarbonate-mediated alkylation of 2,4-dihydroxybenzyaldehyde and 2,4-dihydroxyacetophenone to generate 4-alkylated products in acetonitrile at 80 °C with excellent regioselectivity, up to 95% isolated yields, and broad ...
Cytotoxic and antimicrobial drimane meroterpenoids from a fungus of the Stictidaceae (Ostropales, Ascomycota) [0.03%]
一种Stictidaceae地衣真菌中具有细胞毒性和抗菌活性的Drimanetype meroterpenoids化合物
Laura Flores-Bocanegra,Mario Augustinović,Huzefa A Raja et al.
Laura Flores-Bocanegra et al.
As part of our ongoing research on bioactive fungal metabolites, two new metabolites were isolated from a fungus of the Stictidaceae (strain MSX62440), dasyscyphins F and G (1 and 3), and the known dasyscyphin C (2). Compound 1 was characte...
Mercapto-functionalized polyhedral oligomeric silsesquioxane as a soluble support for the synthesis of peptide thioesters [0.03%]
巯基功能化多面体低聚倍半硅氧烷作为合成肽硫酯的可溶性支持物
Kimberly Perry,Binglin Sui,Yangmei Li
Kimberly Perry
The revival of peptide-based drugs has led to the increasing demand for the development of large-scale synthesis of these complex molecules. To meet this demand, the use of mercapto-functionalized polyhedral oligomeric silsesquioxane (POSS-...