113882-48-7Relevant articles and documents
Visible-Light Photoredox-Catalyzed α-Allylation of α-Bromocarbonyl Compounds Using Allyltrimethylsilane
Gontala, Arjun,Jang, Gwang Seok,Woo, Sang Kook
, p. 506 - 509 (2021)
The development of a greener allylation reagent for α-allylation of carbonyl compounds is of great necessity. Here we present allyltrimethylsilane as a novel allylation reagent in the photoredox-catalyzed α-allylation of carbonyl compounds such as ketones, esters, and amides. The reaction process shows good functional group tolerance and generates a good yield of the product. The reaction mechanism is a radical-mediated reaction by photo-induced single electron transfer.
Triethylborane-Induced Radical Allylation Reaction with Zirconocene-Olefin Complex
Hirano, Koji,Fujita, Kazuya,Shinokubo, Hiroshi,Oshima, Koichiro
, p. 593 - 595 (2004)
(Matrix presented) Allylzirconium reagents are effective for radical allylation of α-halo carbonyl compounds. The key steps would be homolytic cleavage of the zirconium-carbon bond and halogen abstraction by the resulting Cp2ZrCI(III). Zirconoc
Triethylborane-induced radical allylation of α-halo carbonyl compounds with allylgallium reagent in aqueous media
Usugi, Shin-ichi,Yorimitsu, Hideki,Oshima, Koichiro
, p. 4535 - 4538 (2001)
An allylgallium reagent is found to be effective for radical allylation of α-iodo or α-bromo carbonyl compounds. Treatment of benzyl bromoacetate with allylgallium, prepared from allylmagnesium chloride and gallium trichloride, in the presence of triethylborane in THF provided benzyl 4-pentenoate in good yield. The addition of water as a cosolvent improved the yields of allylated products. It was revealed that the allylgallium species resists immediate decomposition on exposure to water.
Diethylzinc-Mediated Radical 1,2-Addition of Alkenes and Alkynes
Li, Xin,He, Songtao,Song, Qiuling
supporting information, p. 2994 - 2999 (2021/05/04)
A novel diethylzinc-mediated radical 1,2-addition of perfluoroalkyl iodides to unactivated alkenes and alkynes is presented, which demonstrates a novel way to generate an ethyl difluoroacetate radical. This method is highly efficient and gives full conversions of the substrates, high yields of the products, and negligible byproducts and requires no column chromatography purifications. The mild conditions enable this protocol to exhibit excellent functional group compatibility.
CYCLOSPORINE COMPOSITIONS AND METHODS OF USE
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Paragraph 0140-0141, (2020/03/15)
Disclosed herein are cyclosporine compounds and methods for use in the treatment or prevention of neutrophil-mediated inflammation, wherein the compounds inhibit the activity of MRP2 and FPR1.
Straightforward synthesis of functionalized (E)-3-acylacrylic acids
Sivák, Ivan,Václav, Jakub,Berke?, Du?an,Kolarovi?, Andrej
supporting information, p. 8871 - 8875 (2015/11/02)
An experimentally simple, mild and straightforward synthetic route towards diversely functionalized (E)-3-acylacrylic acids is described, with Horner-Wadsworth-Emmons (HWE) reaction as the key step. The substrate scope and limitations of the HWE reaction were investigated with a range of β-ketophosphonates. Glyoxylic acid monohydrate was demonstrated to be fully compatible with the HWE reaction conditions, thus avoiding a troublesome hydrolysis of the corresponding 3-acylacrylates in the last step and providing a valuable synthetic shortcut.
METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS
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Paragraph 0618; 0619; 0620, (2014/10/04)
The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H- benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofiiran-3,4-diol and hydrates thereof and methods for treating disorders in which DOTl -mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)- 5 -(((( 1 r,3 S)-3 -(2-(5 -(tert-butyl)- 1 H-benzo[d] imidazol-2- yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
[Cu(dap)2Cl] as an efficient visible-light-driven photoredox catalyst in carbon-carbon bond-forming reactions
Pirtsch, Michael,Paria, Suva,Matsuno, Taisuke,Isobe, Hiroyuki,Reiser, Oliver
supporting information; experimental part, p. 7336 - 7340 (2012/09/08)
Copper sees the light of day: [Cu(dap)2Cl] proved to be an excellent photoredox catalyst for atom-transfer radical addition reactions, as well as for allylation reactions (see scheme), providing an attractive alternative to commonly used iridium- and ruthenium-based catalysts. Copyright
Potassium Channel Modulators
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Page/Page column 38, (2012/05/21)
Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein R1, R2, R3, R4, and R5 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
Targeting the heat shock protein 90 dimer with dimeric inhibitors
Kusuma, Bhaskar Reddy,Peterson, Laura B.,Zhao, Huiping,Vielhauer, George,Holzbeierlein, Jeffrey,Blagg, Brian S. J.
experimental part, p. 6234 - 6253 (2011/10/31)
The design, synthesis, and biological evaluation of conformationally constrained coumermycin A1 analogues are reported. Compounds were evaluated against both breast cancer (SKBr3 and MCF7) and prostate cancer (PC3 mm2, A549, and HT29) cell lines. Non-noviosylated coumermycin A1 analogues that manifest potent antiproliferative activity resulting from Hsp90 inhibition are provided, wherein replacement of the stereochemically complex noviose sugar with readily available piperidine rings resulted in ü100 fold increase in antiproliferative activities as compared to coumermycin A1, producing small molecule Hsp90 inhibitors that exhibit nanomolar activities.