Synthetic studies towards isomeric pyrazolopyrimidines as potential ATP synthesis inhibitors of Mycobacterium tuberculosis. Structural correction of reported N-(6-(2-(dimethylamino)ethoxy)-5-fluoropyridin-3-yl)-2-(4-fluorophenyl)-5-(trifluoromethyl)pyrazolo[1,5- α]pyrimidin-7-amine [0.03%]
合成异构吡唑并嘧啶作为潜在的Mtb ATP合成抑制剂的研究 Structural纠正报道的N-(6-(2-(二甲基氨基)乙氧基)-5-氟吡啶-3-基)-2-(4-氟苯基)-5-(三氟甲基)吡唑并[1,5- α]嘧啶-7-胺结构错误
Peter J Choi,Guo-Liang Lu,Hamish S Sutherland et al.
Peter J Choi et al.
During our studies into preparing analogues of pyrazolopyrimidine as ATP synthesis inhibitors of Mycobacterium tuberculosis, a regiospecific condensation reaction between ethyl 4,4,4-trifluoroacetoacetate and 3-(4-fluorophenyl)-1H-pyrazol-5...
Sequential iodine-mediated diallylsilane rearrangement/asymmetric dihydroxylation: Synthesis and reactions of enantioenriched oxasilacycles [0.03%]
碘介导的二烯基硅烷的重排与非对称双羟化：富集的环氧硅环类化合物的合成及反应性研究
Christopher R Myers,Paul Spaltenstein,Lauren K Baker et al.
Christopher R Myers et al.
Products from an iodine-mediated diallylsilane rearrangement were taken into an asymmetric dihydroxylation (AD) reaction resulting in the formation of diastereomeric 6-membered oxasilacycles. Removal of the epimeric stereocenter among this ...
Matthew S McVeigh,Neil K Garg
Matthew S McVeigh
Transient strained cyclic intermediates, such as strained cyclic allenes, are useful building blocks for the synthesis of structurally and stereochemically complex scaffolds. Trappings of strained cyclic allenes are thought to occur primari...
Kishore Kumar Palli,Palash Ghosh,Shiva Krishna Avula et al.
Kishore Kumar Palli et al.
Remdesivir, the first drug approved by the FDA to treat COVID-19, is in high demand for patients infected with the SARS-CoV-2 virus. Herein, we report a facile approach minimizing the protecting group manipulations to afford remdesivir in g...
Corrigendum to "A click-ready pH-triggered phosphoramidate-based linker for controlled release of monomethyl auristatin E" [Tetrahedron Lett. Volume 61, Issue 41, 8 October 2020, 152398] [0.03%]
对“点击即可使用的pH触发型磷酸胺酯类连接基团实现单甲基奥瑞斯汀E的可控释放”一文的勘误[2020年10月8日出版，卷61，期41，152398]
Feyisola P Olatunji,Jacob W Herman,Brittany N Kesic et al.
Feyisola P Olatunji et al.
[This corrects the article PMC7665082.].
Published Erratum
Tetrahedron letters. 2021 May 11:71:152955. DOI:10.1016/j.tetlet.2021.152955 2021
Refinement of Covalent EGFR Inhibitor AZD9291 to Eliminate Off-target Activity [0.03%]
通过优化共价EGFR抑制剂AZD9291来消除其非专一靶向活化
Elise Bouffard,Balyn W Zaro,Melissa M Dix et al.
Elise Bouffard et al.
Non-small-cell lung cancer (NSCLC) is a major disease that accounts for 85% of all lung cancer cases which claimed around 1.8 billion lives worldwide in 2020. Tyrosine kinase inhibitors (TKIs) that target EGFR have been used for the treatme...
Oxidations of pyrrolidines and piperidines to afford CH-functionalized isopropyl-1-carboxylate congeners [0.03%]
吡咯啶和哌啶的氧化以获得CH官能化异丙基-1-羧酸酯类似物
Steven Gunawan,Nathan Bedard,Christopher Foley et al.
Steven Gunawan et al.
This article describes the action of iodine(III) reagents [diacetoxyiodobenzene, PhI(OAc)2, and iodosobenzene, (PhIO)n] in conjunction with TMSBr which act as functional bromine equivalents in unique oxidations of saturated, carbamate prote...
Reaction between harmaline and vanillin to produce dimeric scaffoldsthat exhibit anti-proliferative activity [0.03%]
harmaline与香草醛反应生成具有抗增殖活性的二聚体支架结构
Vishal C Birar,Gene Zaid,Brian S J Blagg
Vishal C Birar
Herbal medicine is used as a complement to modern medicine for the treatment of human diseases suchas cancer, inflammation, and diabetes. Nutraceutical components in foods such as vanillin produceantioxidant and anticancer activities and ma...
Sophia G Gierszal,Timothy J Barker
Sophia G Gierszal
A reaction between epoxides and benzylboronic acid pinacol esters is described. CuI was found to be an effective catalyst of this transformation upon activation of the benzylboronic ester with an alkyllithium reagent. The reaction was very ...