79027-28-4Relevant articles and documents
Controlled Reduction of Nitriles by Sodium Hydride and Zinc Chloride
Chiba, Shunsuke,Ong, Derek Yiren
, p. 1369 - 1378 (2020/04/27)
A new protocol for the controlled reduction of nitriles to aldehydes was developed using a combination of sodium hydride and zinc chloride. The iminyl zinc intermediates derived from aromatic nitriles could be further functionalized with allylmetal nucleophiles to afford homoallylamines. As the method allows the reduction of various aliphatic and aromatic nitriles with a concise procedure under milder reaction conditions and exhibits wide functional group compatibility, it is well suited for use in various opportunities in chemical synthesis.
SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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, (2017/04/14)
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
Substituted heteroaryl compound and composition thereof, and uses of substituted heteroaryl compound and composition thereof
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, (2017/04/29)
The present invention provides a substituted heteroaryl compound and a composition thereof, and uses of the substituted heteroaryl compound and the composition, wherein the compound is a compound represented by a formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound represented by the formula (I). The present invention further provides a pharmaceutical composition containing the compound, wherein the pharmaceutical composition can regulate activity of protein kinases, particularly Aurora kinases and JAK kinases, and can be used for prevention, treatment, therapy and alleviation of protein kinases, particularly Aurora kinases and JAK kinase activity mediated diseases or disorders.
Ynamide Carbopalladation: A Flexible Route to Mono-, Bi- and Tricyclic Azacycles
Campbell, Craig D.,Greenaway, Rebecca L.,Holton, Oliver T.,Walker, P. Ross,Chapman, Helen A.,Russell, C. Adam,Carr, Greg,Thomson, Amber L.,Anderson, Edward A.
supporting information, p. 12627 - 12639 (2015/09/01)
Bromoenynamides represent precursors to a diversity of azacycles by a cascade sequence of carbopalladation followed by cross-coupling/electrocyclization, or reduction processes. Full details of our investigations into intramolecular ynamide carbopalladation are disclosed, which include the first examples of carbopalladation/cross-coupling reactions using potassium organotrifluoroborate salts; and an understanding of factors influencing the success of these processes, including ring size, and the nature of the coupling partner. Additional mechanistic observations are reported, such as the isolation of triene intermediates for electrocyclization. A variety of hetero-Diels-Alder reactions using the product heterocycles are also described, which provide insight into Diels-Alder regioselectivity.
A formal synthesis of herboxidiene/GEX1A
Yadav, Jhillu S.,Reddy, G. Madhusudhan,Anjum, S. Rehana,Reddy, B. V. Subba
, p. 4389 - 4397 (2014/07/21)
A formal synthesis of herboxidiene/GEX 1A is described. This approach demonstrates successful application of the Prins cyclization for the construction of the tetrahydropyran core of the target molecule. The chirality of the side chain has been established through the Sharpless asymmetric dihydroxylation and Evan's alkylation. The olefin cross-metathesis was applied to couple both key fragments. Copyright
Palladium on charcoal as a catalyst for stoichiometric chemo- and stereoselective hydrosilylations and hydrogenations with triethylsilane
Tuokko, Sakari,Pihko, Petri M.
, p. 1740 - 1751 (2015/02/19)
Stoichiometric quantities of triethylsilane in the presence of activated Pd/C as the catalyst can be used to effect chemo-, regio-, and stereoselective hydrosilylation and transfer hydrogenation reactions. α,β-Unsaturated aldehydes and ketones are selectively hydrosilylated to give the corresponding enol silanes or transfer hydrogenated to give the saturated carbonyl compounds in the presence of other reducible functional groups.
DIHYDROPYRONE COMPOUNDS AND HERBICIDES COMPRISING THE SAME
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, (2014/06/23)
The present invention provides a compound having an excellent efficacy for controlling weeds. A dihydropyrone compound of formula (I): wherein m is 1, 2 or 3; n is an integer of any one of 1 to 5; X represents O, S, S(O) or S(O)2; R1 /sup
Tethered aminohydroxylation: Synthesis of the β-amino acid of microsclerodermins A and B
Pullin, Robert D. C.,Rathi, Akshat H.,Melikhova, Ekaterina Y.,Winter, Christian,Thompson, Amber L.,Donohoe, Timothy J.
supporting information, p. 5492 - 5495 (2013/11/19)
The utility of the tethered aminohydroxylation (TA) has been demonstrated by synthesis of the complex β-amino acid residue of microsclerodermins A and B. The TA provided a regio- and stereoselective functionalization of a complex homoallylic alcohol. The route includes late-stage introduction of the aliphatic side chain via a cuprate addition and cross metathesis, a tactic designed to render the synthesis applicable to other microsclerodermins.
Synthesis of the gymnodimine tetrahydrofuran core through a Ueno-Stork radical cyclization
Toumieux, Sylvestre,Beniazza, Redouane,Desvergnes, Valerie,Araoz, Romulo,Molgo, Jordi,Landais, Yannick
supporting information; experimental part, p. 3726 - 3732 (2011/06/27)
A straightforward access to the C10-C20 skeleton of gymnodimine, incorporating a tetrahydrofuran fragment, is described. The elaboration of the THF moiety is based on a stereocontrolled Ueno-Stork cyclization. A Lewis-acid mediated allylation of the resulting acetal at C13 and a Horner-Wadsworth-Emmons olefination on the ketone at C17 complete the synthesis.
Palladium-catalyzed cascade cyclization of ynamides to azabicycles
Greenaway, Rebecca L.,Campbell, Craig D.,Holton, Oliver T.,Russell, C. Adam,Anderson, Edward A.
supporting information; scheme or table, p. 14366 - 14370 (2012/02/04)
Cascade reactions: A modular assembly of azabicycles by using a cascade cyclization/Suzuki coupling/6π-electrocyclization of bromoenynamides is reported (see scheme). The reaction offers a wide substituent scope on the bicyclic aminodiene products, which can be selectively oxidized as a general approach to aromatic azabicycles.
