- Optimization of physicochemical properties is a strategy to improve drug-likeness associated with activity: Novel active and selective compounds against Trypanosoma cruzi
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Trypanosoma cruzi is the causing agent of Chagas disease, a parasitic infection without efficient treatment for chronic patients. Despite the efforts, no new drugs have been approved for this disease in the last 60 years. Molecular modifications based on
- Amaral, Maiara,Romanelli, Maiara M.,Tempone, Andre G.,Varela, Marina T.,de Castro Levatti, Erica V.,Fernandes, Jo?o Paulo S.
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- Introduction of the 4,4,4-Trifluorobut-2-ene Chain Exploiting a Regioselective Tsuji-Trost Reaction Catalyzed by Palladium Nanoparticles
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A palladium-nanoparticle-catalyzed Tsuji-Trost reaction of 4,4,4-trifluorobut-2-en-1-yl acetate and ethyl(4,4,4-trifluorobut-2-en-1-yl)carbonate was accomplished with various nucleophiles including phenols, amines, and malonates. In the case of the phenols, isomerization of the double bond in the product (up to 20%) was observed as a side reaction. Further synthetic transformations including hydrogenation, the Diels-Alder reaction, and asymmetric dihydroxylation of a product were also examined.
- Hemelaere, Rémy,Desroches, Justine,Paquin, Jean-Fran?ois
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supporting information
p. 1770 - 1773
(2015/04/14)
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- Ruthenium-catalyzed linear selective allylic aminations of monosubstituted allyl acetates
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The ruthenium-catalyzed highly linear selective allylic amination of monosubstituted allylic acetates with secondary amines was developed. The regioselectivity was controlled by the Ru3(CO)12/2-DPPBA catalyst, and a linear-type aminated product was obtained as a single regioisomer.
- Kawatsura, Motoi,Ata, Fumio,Hirakawa, Takuya,Hayase, Shuichi,Itoh, Toshiyuki
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p. 4873 - 4875
(2008/09/21)
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- Iridium complex-catalyzed allylic amination of allylic esters
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Iridium complex-catalyzed allylic amination of allylic carbonates was studied. The solvent strongly affected the catalytic activity. The use of a polar solvent such as EtOH is essential for obtaining the products in high yield. The reaction of (E)-3-substituted-2-propenyl carbonate and 1-substituted-2-propenyl carbonate with pyrrolidine in the presence of a catalytic amount of [Ir(COD)Cl]2 and P(OPh)3 (P/Ir=2) gave a branch amine with up to 99% selectivity. Both secondary and primary amines could be used for this reaction. When a primary amine was used, selective monoallylation occurred. No diallylation product was obtained. The reaction of 1,1-disubstituted-2-propenyl acetate with amines exclusively gave an α,α-disubstituted allylic amine. This reaction provides an alternative route to the addition of an organometallic reagent to ketimines for the preparation of such amines. The reaction of (Z)-3-substituted-2-propenyl carbonate with amines gave (Z)-linear amines with up to 100% selectivity. In all cases, no (E)-linear amine was obtained. The selectivities described here have not been achieved in similar palladium complex-catalyzed reactions.
- Takeuchi,Ue,Tanabe,Yamashita,Shiga
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p. 9525 - 9534
(2007/10/03)
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- Palladium(0)-Catalyzed Substitution of Allylic Substrates in an Aqueous-Organic Medium
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A palladium(0)-water soluble catalyst prepared in situ from palladium acetate and the sulfonated triphenyl phosphine P(C6H4-m-SO3Na)3 (or tppts) is an efficient catalyst for allylic substitution with various carbon and heteronucleophiles in an aqueous-organic medium, allowing a very easy separation of the product(s) and the recycling of the catalyst.
- Blart, Errol,Genet, Jean Pierre,Safi, Mohamed,Savignac, Monique,Sinou, Denis
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p. 505 - 514
(2007/10/02)
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- Generation of Aminyl Radicals using Sulfenamides as Synthetic Precursors
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Sulfenamides are synthesised from reaction between amines and N-(benzenesulfenil)-phthalimide or benzenesulfenyl chloride.The sulfenamides undergo reaction with tributyltin hydride to yield aminyl radicals which can be cyclised onto suitable alkenes. Key Words: sulfenamides; aminyl radicals; tributyltin hydride; radical-cyclisation; N-(benzenesulfenyl)phthalimide
- Bowman, W. Russell,Clark, David N.,Marmon, Robert J.
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p. 1275 - 1294
(2007/10/02)
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