A5008953398- Chemical Synthesis and Analysis
- Synthesis and Biological Evaluation
- Synthesis of heterocyclic compounds
- Microwave-Assisted Synthesis and Applications
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Trypanosoma species research and implications
- Research on Leishmaniasis Studies
- Synthesis and biological activity
- Organophosphorus compounds synthesis
- Synthesis and Reactions of Organic Compounds
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Characterization of Heterocyclic Compounds
- Polyamine Metabolism and Applications
- Chemical Reactions and Isotopes
- Advanced Synthetic Organic Chemistry
- Chemical Synthesis and Reactions
- Multicomponent Synthesis of Heterocycles
- Quinazolinone synthesis and applications
- Chemical Reactions and Mechanisms
- Parasites and Host Interactions
- Catalytic Cross-Coupling Reactions
- Carbohydrate Chemistry and Synthesis
- Asymmetric Hydrogenation and Catalysis
Consejo Nacional de Investigaciones Científicas y Técnicas
2009-2024
University of Buenos Aires
2011-2024
Universidade de São Paulo
2024
Universidade Estadual de Campinas (UNICAMP)
2021-2024
Chagas disease (CD), caused by the flagellate protozoan Trypanosoma cruzi, is a neglected tropical endemic in 21 countries. The only two antiparasitic drugs approved for its treatment, benznidazole and nifurtimox, have significant drawbacks. We present herein optimization of series substituted indoles that were identified through phenotypic screening against T. cruzi. Early lead compounds with balanced potency physicochemical properties advanced to animal studies but showed limited plasma...
The first general procedure for the synthesis of 5- to 7-membered cyclic iminoethers by microwave-assisted cyclization ω-amido alcohols promoted polyphosphoric acid (PPA) esters is presented. 2-Aryl-2-oxazolines and 5,6-dihydro-4H-1,3-oxazines were efficiently prepared using ethyl polyphosphate/CHCl3. Trimethylsilyl polyphosphate in solvent-free conditions allowed hitherto-unreported 4,5,6,7-tetrahydro-1,3-oxazepines. method involves good excellent yields short reaction times.The mechanism...
The first general procedure for the synthesis of 5 to 7-membered 1-aryl-2-iminoazacycloalkanes is presented, by microwave-assisted ring closure ω-arylaminonitriles promoted polyphosphoric acid (PPA) esters. 1-Aryl-2-iminopyrrolidines were easily prepared from acyclic precursors employing a chloroformic solution ethyl polyphosphate (PPE). use trimethylsilyl (PPSE) in solvent-free conditions allowed 1-aryl-2-iminopiperidines and hitherto unreported 1-aryl-2-iminoazepanes. cyclization reaction...
N-Substituted 1,4-diaminobutane (putrescine) and 1,5-diaminopentane (cadaverine) derivatives are of biochemical pharmacological interest as synthetic analogs natural polyamines.1 Several der...
Abstract An efficient microwave protocol is described for the Michaelis–Arbuzov synthesis of secondary and tertiary N-aryl (and alkyl) (diethylphosphono)acetamides 1, by reaction chloro- bromoacetamides with triethyl phosphite in presence catalytic amounts sodium iodide. Remarkable acceleration (minutes vs. several hours) over conventional heating was achieved, together improved product yields purity, when were employed as substrates. Chloroacetamides comparatively less reactive, leading to...
A general procedure for the synthesis of 2-substituted tetrahydro-1,3-thiazepines by MW-assisted cyclization 4-thioamidobutanols is presented. The acyclic precursors were prepared in high overall yields an expeditious three-step diacylation/thionation/deprotection sequence from 4-aminobutanol. Microwave-assisted ring closure 4-thioamido alcohols promoted trimethylsilyl polyphosphate (PPSE) solvent-free conditions allowed several hitherto unreported seven-membered iminothioethers bearing...
An efficient and general method for the synthesis of 2-substituted thiazolines 5,6-dihydro-4H-1,3-thiazines is developed via microwave-assisted ring closure ω-thioamidoalcohols promoted by ethyl polyphosphate (PPE). The cyclization reaction involves an SN2-type mechanism features advantages very short times, high yields a predictable stereochemical outcome. acyclic precursors are prepared in overall improved diacylation–thionation–saponification sequence from commercially available...
Chagas disease (CD) is a parasitic neglected tropical (NTD) caused by the protozoan
Abstract via N‐alkylation of aryl amines with ω‐haloalkyl nitriles (I) followed by reduction the crude amination products
Abstract Polyphosphate‐promoted, microwave‐assisted cyclization of appropriate ω‐arylaminonitriles provides access to corresponding 1‐aryl‐2‐iminopyrrolidines (II), ‐2‐iminopiperidines (IV) and hitherto unreported ‐2‐iminoazepanes (VI).
Selectively N-substituted 1,4-diaminobutane (putrescine) and 1,5-diaminopentane (cadaverine) derivatives are of biochemical pharmacological interest as synthetic analogs natural polyamines. Several have been described acting antibiotics, antineoplastics, antiparasitic agents, NMDA or cholinergic modulators. In addition, such compounds represent key intermediates for acyclic heterocyclic polyamine derivatives.N-Aryl putrescines cadaverines a challenge, since the available methods di...
Abstract Chloroacetamides are significantly less reactive than bromoacetamides.
A general procedure for the synthesis of 2-substituted tetrahydro-1,3-thiazepines is presented, by MW-assisted cyclization 4-thioamidobutanols. The acyclic precursors were prepared in high overall yields an expeditious three step diacylation/thionation/deprotection sequence from 4-aminobutanol. Microwave assisted ring closure 4-thioamidoalcohols promoted trimethylsilyl polyphosphate (PPSE) solvent-free conditions allowed several hitherto unreported seven-membered iminothioethers bearing...