Publications (41) View all
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Article: Palladium-Catalyzed Cross-Coupling Reaction of Thioglycosides with (Hetero)aryl Halides
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ABSTRACT: Abstract: a- and b-thioglycosides serve as effective nucleophiles for Buchwald–Hartwig cross-coupling reactions using functionalized (hetero)aryl halides. The functional group tolerance on the electrophilic partner is typically high, both benzyl and acetate protecting groups on the carbohydrate are tolerated, and anomer selectivities of thioglycosides are high in all cases studied. The efficiency of this general protocol was well demonstrated by the synthesis of 4- methyl-7-thioumbelliferyl-b-d-cellobioside (MUSCB).Advanced Synthesis & Catalysis 02/2013; 355(2-3):477. · 6.05 Impact Factor -
Article: Cs2CO3 in pyrrolidinone promoted hydration of functionalized (hetero)aryl nitriles under metal-free conditions
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ABSTRACT: An efficient hydration reaction of various (hetero)aryl nitriles using Cs2CO3 in pyrrolidinone is described. This new metal-free protocol proved to be highly effective and general to synthesize a variety of (hetero)aryl amides.Tetrahedron Letters 06/2012; 52(23):2860. · 2.68 Impact Factor -
Article: Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives.
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ABSTRACT: A new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure-activity relationship studies enabled identification of compounds 3a and 4g as the most active compounds against L. donovani promastigotes and amastigotes parasites (IC(50) values in a range of 2-11 μM). Additionally, compound 3b has emerged from this study as the most active compound in the series against T. b. brucei with a MEC value of 12 μM. These three compounds are worth of further in vivo evaluation.European journal of medicinal chemistry 03/2012; 52:44-50. · 3.27 Impact Factor -
Article: Palladium-catalyzed decarboxylative coupling of quinolinone-3-carboxylic acids and related heterocyclic carboxylic acids with (hetero)aryl halides.
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ABSTRACT: An efficient and practical decarboxylative cross-coupling reaction of quinolin-4(1H)-one 3-carboxylic acids with (hetero)aryl halides has been established. Under a bimetallic system of PdBr(2) and silver carbonate, the protocol proved to be general, and a variety of 3-(hetero)aryl 4-quinolinones and related heterocycles, such as 3-aryl-1,8-naphthyridin-4(1H)-ones, 3-arylcoumarins, 3-arylquinolin-2(1H)-ones, and 2-arylchromones, can be prepared in good to excellent yields.Organic Letters 03/2012; 14(6):1496-9. · 5.86 Impact Factor -
Article: Copper-Catalyzed Direct Amination of Halo(hetero)arenes with Sodium Azide as the Amino Source
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ABSTRACT: In the synthesis of primary (hetero)aryl amines through copper-catalysis, the ammonia surrogates or aqueous ammonia nucleophilic partners can be replaced by sodium azide. Recent efforts in copper-mediated transformation of (hetero)aryl halides to (hetero) aryl amines using azide anion as the amino source are discussed in these highlights.Mini-Reviews in Organic Chemistry 10/2011; 8(4):448-454. · 2.41 Impact Factor
