Efficient total synthesis of three alpinoids via the Au(I)-catalyzed Meyer-Schuster rearrangement [0.03%]
通过Au(I)催化的Meyer-Schuster重排高效合成三种alpinoids类化合物
Jasmine K Keyes,Mauri B Butzke,Kenneth A Miller
Jasmine K Keyes
The total syntheses of three structurally related natural products, deoxyalpinoid B, deoxyalpinoid A, and alpinoid F, are reported, and each features a Au(I)-catalyzed Meyer-Schuster rearrangement as the key step. The synthesis of alpinoid ...
RECENT ADVANCES IN BASE METAL-CATALYZED COOPERATIVE TRANSFER HYDROGENATION AND HYDRODEUTERATION OF ALKENES [0.03%]
近来金属催化的不饱和键的协同转移氢化和氢去质子化反应的研究进展
Hai N Tran,Julian G West
Hai N Tran
Catalytic alkene hydrogenation is a powerful method that has been widely used in the syntheses of valuable products ranging from commodity chemicals to pharmaceuticals. Hydrogenation has also been a key strategy for selectively introducing ...
The full spectrum tuning of fluorescent molecules via a one-pot multicomponent reaction [0.03%]
一锅多组分反应实现荧光分子的全谱调谐
Nathan Bedard,Addison G Coen,Scott Pekarske et al.
Nathan Bedard et al.
Fluorogenic probes for imaging enable visualization and analysis of difficult-to-reach cells and organelles. However, there are limited efficient examples of tuning these fluorescent molecules to higher wavelengths. This is vital since diff...
Synthesis of the Hypoxia-Inducible Factor-2 α (HIF-2 α) Inhibitor, 3-[(1 S,2 S,3 R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977, Belzutifan); Efficient Replication of Established Approaches [0.03%]
缺氧诱导因子-2 α (HIF-2 α) 抑制剂 3-[(1S,2S,3R)-2,3-二氟-1-羟基-7-甲磺酰基茚-4-基]氧-5-氟苯腈 (PT2977, Belzutifan) 的合成；已建立方法的有效复制
Khagendra B Hamal,Cyprian I Pavlich,Graham J Carlson et al.
Khagendra B Hamal et al.
A concise linear synthesis of hypoxia inducible factor-2α (HIF-2α) inhibitor, belzutifan was achieved by reproducing key components of previous synthetic approaches to this molecule as described in several publications and patents. Belzut...
Semisynthesis, Characterization, and Biological Evaluation of Fluorinated Analogues of the Spirobisnaphthalene, Diepoxin-η [0.03%]
氟化Spirobisnaphthalene（Diepoxin-η）类似物的半合成、表征和生物评价
Hadi Pourhadi,Tamam El-Elimat,Manuel Rangel-Grimaldo et al.
Hadi Pourhadi et al.
Diepoxin-η (1) is a cytotoxic fungal metabolite belonging to the spirobisnaphthalene structural class. In this study, four mono fluorinated analogues (2-5) of diepoxin-η (1) were semisynthesized in a single-step by selectively fluorinatin...
4-Isocyanoindole-2'-deoxyribonucleoside (4ICIN): An Isomorphic Indole Nucleoside Suitable for Inverse Electron Demand Diels-Alder Reactions [0.03%]
4-异氰基吲哚-2'-脱氧核苷(4ICIN)：一种适合逆电子需求狄尔斯- Alder反应的异吲哚核苷
Kellan T Passow,Daniel A Harki
Kellan T Passow
Isomorphic nucleosides are powerful tool compounds for interrogating a variety of biological processes involving nucleosides and nucleic acids. We previously reported a fluorescent isomorphic indole nucleoside called 4CIN. A distinguishing ...
Carboxyl activation via silylthioesterification: one-pot, two-step amidation of carboxylic acids catalyzed by non-metal ammonium salts [0.03%]
通过硅基硫酯的羧基活化反应催化非金属铵盐一步两步胺形成酸
Angus A Lamar,Lanny S Liebeskind
Angus A Lamar
The first organo-catalyzed silylthioesterification of a carboxylic acid and a commercially available mercaptoorganosilane results in the in situ production of an O-silylthionoester. Subsequent amine addition forms amides in an operationally...
Computational study of an oxetane 4 H-pyrazole as a Diels-Alder diene [0.03%]
作为Diels-Alder双烯体的氧杂环丁基4H吡唑的计算研究
Brian J Levandowski,Nile S Abularrage,Brian J Graham et al.
Brian J Levandowski et al.
We combine the effects of spirocyclization and hyperconjugation to increase the Diels-Alder reactivity of the 4H-pyrazole scaffold. A density functional theory (DFT) investigation predicts that 4H-pyrazoles containing an oxetane functionali...
Palladium-catalyzed allylation of 2- and 4-alkylpyridines via N-allyl alkylidene dihydropyridine intermediates [0.03%]
钯催化下通过N-烯丙基烯二醇缩合物介导的吡啶
Grant N Shivers,F Christopher Pigge
Grant N Shivers
A method to introduce allyl or cinnamyl groups to the picolyl positions of 2- or 4-alkylpyridines is described. Substituted N-allyl pyridinium salts are first treated with base (KOtBu) followed by catalytic [(η3-allyl)PdCl]2 and PPh3 to re...
Vincent van der Puyl,Ruairi O McCourt,Ryan A Shenvi
Vincent van der Puyl
Earth abundant metal catalysts hold advantages in cost, environmental burden and chemoselectivity over precious metal catalysts. Differences in reactivity for a given metal center result from ligand field strength, which can promote reactio...