10^th European Organic Chemistry Congress March 21-22, 2019 Hotel Holiday Inn, Aurelia Rome, Italy

Biography:

Mangalagiu is a professor of organic and medicinal chemistry and Vice-Rector with research at Alexandru Ioan Cuza University of Iasi, Romania. Previously, prof. Mangalagiu served as Dean, Vice-Dean, Head of Organic Chemistry Department, etc. at Faculty of Chemistry. He has nearly 30 years of experience in the research, focused in the area of Heterocycles Compounds. He has over 150 papers, 13 patents, 3 international chapter books, etc. He was Visiting Professor and/or invited speaker to prestigious foreign universities (Ludwig Maximilianus University Munchen and Technische Universität  Braunschweig, University of Florence, Universite D’Angers), awarded with numerous prizes and honours: DAAD and NATO award, “Costin D. Nenitescu Medal” (Romanian Society of Chemistry), “Al.I.Cuza University Award in Research”, Special Award of Croatian Association of Inventors, etc.

Abstract:

During the last fifty years, nitrogen heterocycles compounds have received considerable attention as highly valuable  materials in the fields of pharmacy /  medicine, opto-electronics and agriculture.As part of our ongoing research in the field of azaheterocycles derivatives, we present herein some core results obtained by our group in the field of nitrogen heterocycles derivatives, focused on chemistry and their pharmacological and industrial potential applications.

The chemistry presented is straight and efficient, and focused in the area  diazols, triazols, azine (and bis-azine), diazine (and bis-diazine), phenanthroline and related. Stereo- and regio- chemistry aspects are discussed. The chemistry involve both conventional (thermal heating) and nonconventional (microwave and ultrasounds) methods.Concerning pharmacological potential applications,  our attention was focused in the area of obtaining compounds with anticancer, antimycobacterial, anti-leishmanial, and other antimicrobials activity.

For the industrial potential applications our research was focused in obtaining of new chemical entities with fluorescent property, molecular devices (such as logic gates), chemosensors, growth regulators for plants, pesticides and insecticides, ionic liquids for synthetic uses.

Biography:

Vincent Dalla completed his PhD in 1994 at the University of Reims Champagne-Ardennes. In 1995 he was appointed “Maitre de Conferences” at the Ecole Nationale Supérieure de Chimie de Lille, and then in 1999 he moved to the University of Le Havre, where he became professor in 2008. His main research interests include the development of catalytic, stereoselective, and tandem reactions in N-acyliminium ion chemistry and their synthetic applications towards alkaloid type structures.

Abstract:

Over the last decade my research group developed some efficient catalytic methodologies in the area of N-acyliminium ion chemistry. Those methods are largely contingent to the use of Brønsted and Lewis superacidic catalysts of the triflate and triflimidate family to activate and enable effective alkylations of cyclic N,O-acetals as N-acyliminium precursors. Driven by the current societal stakes to develop sustainable chemistry with the respect of atom- and step economy principles as the guidelines, recently we particularly endeavored to integrate our catalytic N-acyliminium processes into more complex, sequential events. This talk will illustrate our efforts in designing cascade and multicatalytic transformations that provide a wide array of relatively sophisticated polyanellated structures from trivial cyclic N,O-acetals with general good efficiency.

Biography:

Abstract:

Control over crystallization plays a very important part in the process development of Active Pharmaceutical Ingredients (APIs). The use of Process Analytical Technology (PAT) tools such as Focused Beam Reflectance Measurement (FBRM) and Particle Vision and Measurement (PVM) allows an in-line analysis of on-going crystallizations and evaluate in real-time the crystals size and morphology. These latter properties are fundamental to achieve a good filtration, ensuring displacement of solvents and impurities, for shorter drying times and for formulation (grinding, milling, etc).

The principles of these two technologies will be summarized and case study examples will be presented showcasing the application of FBRM and PVM probes in the development of crystallization processes at Hovione. The use of these technologies has become a standard of best practices in our process development and inserted in our work-flow of Excellent Development and Manufacturing (EDaM).

Biography:

Abstract:

Alzheimer’s disease (AD) is widely believed to be related to the production and deposition of the beta-amyloid (Aβ). Thus, beta-amyloid cleaving enzyme (BACE1) inhibitors, that can reduce the production of the Aβ peptide, are promising candidates for the treatment of AD. Pfizer researchers discovered a potent, selective BACE1 inhibitor that displayed good safety, tolerability, and pharmacokinetics from early stage clinical trials. The compound also exhibited excellent brain penetration, and potent in vivo efficacy. The exploratory active pharmaceutical ingredient (API) support strategy and the process development will be discussed. In this presentation, the synthesis of the complex target molecule will encompass the greening of a chiral isoxazoline production, continuous flow chemistry of a critical heteroaryl bromide-metal exchange and telescoped heteroaryl anion addition, and the GMP endgame development in multiple clinical campaigns.

Biography:

Njomza Ajvazi has completed her BSc and MSc in the field of Organic Chemistry with Biochemistry at the University of Prishtina "Hasan Prishtina", Kosovo, in 2009. Her Doctor of Science degree was conferred by Jožef Stefan International Postgraduate School, Ljubljana, Slovenia, in 2016, under the supervision of Professor Dr. Stojan Stavber. Currently, she is an Assistant Professor at the College of Medical Sciences "Rezonanca", and Teaching Assistant at the Faculty of Agriculture and Veterinary at the University of Prishtina "Hasan Prishtina", Kosovo. Her research interest is the development of new methodologies for comprehensive direct transformation of alcohols forming new C-C or C-heteroatom bonds under green reaction conditions.

Abstract:

Nucleophilic substitution of alcohols leading to the construction of the C-C bond following the principles of green chemistry has become an attractive process used in the synthesis of organic compounds. Because increasing numbers of organic solvents are restricted due to their damaging effects on human health and the environment, performing reactions under solvent-free reaction conditions (SFRC), have attracted significant interest in organic chemistry research and development because of their simplicity and cost efficiency. C-C bond construction reactions display one of the most important implements in synthetic organic chemistry since they provide access to pharmaceutically important molecules or agrochemicals. C-C bond construction by direct cross-coupling of alcohols with C-nucleophiles could be a desirable strategy offering a potential impact on the environment since water is the only by-product of the reaction. Hydroxyl functional group is one of the most abundant in organic compounds. In order to manipulate a specific transformation of a hydroxyl moiety, often its activation is necessary, but in some cases, its direct substitution is also possible. Numerous related methodologies have been elaborated employing a sub-stoichiometric amount of Bronsted acids, metals ions, Lewis/Bronsted acid combination or other promoters. However, these reactions involve either toxic or expensive reagents, environmentally undesirable solvents, a high concentration of the catalyst, prolonged reaction time or high temperature. Thus, the development of an efficient, selective and environmentally benign catalytic methodology for C-C bond construction remains an attractive research challenge. A group of organic molecules bearing an active N-halogen bond: N-halosuccinimides (chloro, bromo or iodo respectively), are an inexpensive, commercially available and metal-free reagents which are widely used in organic synthesis as oxidizing, hydroxy halogenating or halogenating agents. We report new, efficient and selective methodology for the direct cross-coupling of alcohols with C-nucleophiles catalyzed by N-halosuccinimide as metal-free catalyst under SFRC, enhancing the green chemical profiles of these transformations.

Biography:

Eyad Mazin Mallah has completed his PhD at Tuebingen University, Germany. He is currently working as an Associate Professor and Dean’s Assistant in the Faculty of Pharmacy at the University of Petra. He has a specific interest in Pharmaceutical Organic Chemistry and Pharmaceutical Analytical Chemistry. Currently, he is working on development of chromatographic and immunoassay methods for analyzing different pharmaceutical compounds in biological fluids which could be used in bio-studies. In addition, he is interested in drug-drug interactions and drug-juice interactions which could affect the pharmacokinetic profile of some pharmaceutical products. He is also working on the synthesis of some Barbituric acid and Imidazole derivatives and their application in pharmaceutical compounds. He has published about 50 articles in different international journals.

Abstract:

Biography:

E.-E. Vlachou has completed her MSc at the age of 25 years from Aristotle University, Department of Chemistry, in Organic Synthesis. Now she continues her studies as a PhD student at the same field. She has participated in many conferences and she has published two papers in Journal of Heterocyclic Chemistry and in Bioorganic Chemistry until now.

Abstract:

Dipetalolactone and 4-methyldipetalolactone are prepared in excellent yield by a one-pot tandem propargylation/Claisen rearrangement/cyclization reaction of the corresponding 5,7-dihydroxycoumarins with 3-chloro-3-methylbut-1-yne in the presence of Cs₂CO₃ under microwave irradiation. The analogous reactions of propargyl chloride with esculetins or 5,7-dihydroxy-coumarins led to dipropargyloxy derivatives. The later by treatment with gold nanoparticles supported on TiO₂ or BF₃.Et₂O in DMF, under microwave irradiation resulted in very good to excellent yield to the corresponding fused dipyranocoumarins. The reactions of esculetins with 3-chloro-3-methylbut-1-yne gave mainly exo-methylene fused dioxino[g]coumarins.

The reactions of 6-amino-7-hydroxycoumarins and 7-amino-6-hydroxycoumarins with propargyl bromide and 3-chloro-3-methylbut-1-yne in the presence of Cs₂CO₃ under microwave irradiation led to dipropargyl derivatives. The latter by treatment with gold nanoparticles supported on TiO₂ or BF₃.Et₂O in DMF, under microwave irradiation resulted to the corresponding fused pyrido-pyranocoumarins. The new compounds were tested in vitro for their antioxidant and antiinflammatory activities.

Biography:

Ani H Hasratyan has obtained her Master’s degree in Chemical Faculty at Yerevan State University in 2013 under supervision of T Ghochikyan. She received her PhD in 2017 under the supervision of Dr M Sargsyan. During her scientific work she has already done a lot of experiments and has 24 published articles. Her research interest is NMO/H2O system and its chemical properties in applied organic synthesis. She participated in several national and international conferences.

Abstract:

It is known from literature that 1-vinylimidazole, when interacting with transition metal chlorides, forms donor-acceptor complexes due to the free pair of electrons of nitrogen atoms in position 3 and the vacant metal orbital. Coordination compounds of gold+3 with 1-vinylimidazole, in contrast to transition metal complexes, are not known in the literature. In this work, we first investigated the interaction of HAuCl4 with 1-vinylimidazole, which, in turn, was synthesized in the NMO/H2O system without the use of explosive acetylene. The X-ray diffraction analysis showed that, in the crystal structure, the AuCl4– poly anions bind to the vinyl imidazole molecules (C5H7N2)+1 by hydrogen bonds of the Cl ••• H–C and Cl ••• Н-N types forming infinite chains alternating in the direction. The vinyl fragment of 1-vinylimidazole is not involved in coordination.

Biography:

Xiaolong Liu has completed his PhD at Zhejiang University. Currently, he is working as an Assistant Professor at the Institute of Process Engineering, Chinese Academy of Sciences. He has published more than 15 papers in reputed journals. His research interests mainly focus on the catalytic oxidation of organic pollutants, such as VOCs (volatile organic compounds) & POPs (persistent organic pollutants).

Abstract:

Volatile organic compounds (VOCs) emitted from the industrial plants are toxic and are dangerous to human health. Among the abundant VOCs pollutants, chlorinated volatile organic compounds (OVOCs), including chlorobenzene (CB), dichloromethane (DCM), 1, 2-dichloroethane (DCE), and trichloroethylene (TCE), are regarded as an important group of VOC pollutants due to its high toxicity, strong stability, and poor reactivity. In comparison to other noble metals (Pd, Pt, Rh), Ru catalysts have been far less explored in environmental catalysis. Recently, Ru catalysts have been well demonstrated in catalytic oxidation of alkanes, alkenes, aromatics, and some halogenated volatile organic compounds. In this work, noble metal catalysts (Pd, Pt, Ru, and Rh) were prepared and evaluated in the catalytic oxidation chlorobenzene, and Ru/TiO₂ contributed the best catalytic performance. During the oxidation, polychlorinated benzenes PhCl_x (x≥2) were observed, and Ru/TiO₂ showed apparently lower PhCl_x concentrations than other three samples. Besides, the dioxin-like PCBs (dl-PCBs) were collected and analyzed for Pd/TiO₂ and Ru/TiO₂. The ∑dl-PCBs produced by Pd/TiO₂ was about 1.5 times that of Ru/TiO₂. XPS analyses revealed that Ru/TiO₂-used gave the lowest Cl content among the used catalysts, and the lowest (Cl_ad+Cl_or)/Cl value and the highest Cl_br/Cl value, which might be an important reason for its strongest chlorine removal ability and the lowest yields of polychlorinated by-products. In-situ FTIR studies were also conducted for Pd, Pt, Ru, and Rh catalysts, and various organic intermediates were observed on the catalyst surface. Besides, density functional theory (DFT) was also conducted to investigate the main reason for the difference of the catalytic performance of Ru and other three samples (Pd, Pt, and Rh). Accordingly, a reaction mechanism for the catalytic oxidation of chlorobenzene was proposed

Biography:

Alexander O Terent’ev has received his MS in Chemistry of Biologically Active Compounds at D. Mendeleev University of Chemical Technology of Russia, Moscow; PhD and DSc in Organic Chemistry in N.D. Zelinsky Institute of Organic Chemistry RAS in 2000 and 2009 respectively. Currently, he is the Head of laboratory at N D Zelinsky Institute of Organic Chemistry RAS and Head of laboratory at All-Russian Research Institute of Phytopathology. His interests are Organic Chemistry, Medical and Agricultural Chemistry, Chemical Technology. He published three chapters in books, 110 research papers, and 30 patents.

Abstract:

Oxidative cross-dehydrogenative coupling is included in the modern trends of organic chemistry. It eliminates necessity for introduction of additional functional groups and affords direct coupling in one stage (via selective C-H activation) with limited amount of wastes, high atom- and step- economy. Oxidative cross-dehydrogenative C-C coupling was studied in most detail; the C-N, C-P, and C-O cross-coupling reactions are less developed. The problem is in achieving of high selectivity in the cross-dehydrogenative C-O coupling because the starting compounds are prone to side oxidation and fragmentation reactions producing, for example, alcohols and carbonyl compounds. This gives rise to a problem of searching for oxidizing agents and reaction conditions suitable for the cross-coupling of different types of substrates. We discovered oxidative cross-dehydrogenative C-O coupling of 1, 3-dicarbonyl compounds, their heteroanalogs, and heterocycles with peroxides, oximes and hydroxyamides. The best results were obtained with the use of the widely available copper, iron, manganese or lanthanide salts as catalysts or oxidants.

Biography:

Paweł Woźnicki was born in 1990. In 2017 he obtained his bachelor's degree in chemistry from Maria Curie-Skłodowska University in Lublin where he has been conducting research under the supervision of Professor Marek Stankevič. In 2017 he received Scholarship of Minister of Science and Higher Education. In 2018 he was awarded "Diamond Grant", an annual grant awarded by the Polish Minister of Science and Higher Education to students holding a bachelor's or engineer's degree. Currently he continues his research as a doctoral student. His academic interests include synthesis of organophosphorus compounds, stereoselective synthesis and transition metal-catalyzed transformations.

Abstract:

Organophosphorus compounds are one of the main classes of ligands used in transition metal-catalyzed reactions such as cross-coupling, catalytic hydrogenation and olefin metathesis. Among them cycloalkyl and P-heterocyclic phosphines constitute an important subgroup with good σ-donating ability and medium to high steric hindrance, these properties render them suitable for palladium- and nickel-catalyzed cross-coupling of less reactive or deactivated substrates such as aryl chlorides with electron-donating substituents, aryl sulfonates, aryl carboxylates, and aryl ethers.

We have developed a new method of the synthesis of cyclic di- and monoarylphosphine derivatives through haloalkylation of simple secondary or tertiary phosphine-boranes and sulfides followed by α-metallation and intramolecular nucleophilic substitution of halide at the terminal carbon atom. Depending on the properties of the phosphorus group and the length of the haloalkyl substituent monoarylphosphine derivatives led to the formation of P-cycloalkyl or P-heterocyclic products. The use of chiral butyllithium-sparteine base allowed the formation of chiral non-racemic cycloalkylphosphine analogues which were used to synthesize diphosphine ligand precursors via iron-mediated homocoupling.

Biography:

Abstract:

Clarithromycin is Macrolides. is a semisynthetic 14-membered ring macrolide antibiotic. Clarithromycin binds to the 50S ribosomal subunit and inhibits RNA-dependent protein synthesis in susceptible organisms.

Metronidazole is a Nitro- imidazole Antimicrobial. The chemical classification of metronidazole is Nitro-imidazole. Metronidazole is a synthetic nitro-imidazole derivative with antiprotozoal and antibacterial activities.

The pomegranate (Punica granatum) is a fruit-bearing deciduous shrub or small tree in the family Lythraceae that grows between 5 and 10 m (16 and 33 ft.) tall

A simple, reproducible and rapid analytical method by using high performance liquid chromatography-mass spectrometry (HPLC/MS) with high resolution and sensitivity for simultaneous quantification of Clarithromycin and Metronidazole in presence of pomegranate juice was validated. A gradient mobile phase system consisting of methanol and 0.1% of formic acid and ACE 5 C18 column (50 X 2.1 mm, 5μ) were used with a flow rate of 1.0 ml/ min.

An acceptable recovery was achieved (97.75%) and (96.0%) for Clarithromycin and Metronidazole, respectively, with good accuracy and precision. Coefficient of determination (R²) of the standard curves for both drugs ranged between 0.9986 and 0.9998.

According to results obtained, there was no significant effect on pharmacokinetic parameters of Clarithromycin after pre-treatment with single and multiple doses of pomegranate fresh juice. However, there was two hours-long delay on T-max after the single dose of juice which is possibly with no clinically significant. Furthermore, the changing in t½ and the elimination rate constant of Clarithromycin after single and multiple pomegranate juice administration gives an expectation that pomegranate juice could affect the hepatic-mediated metabolism of Clarithromycin but with insignificant manner.

Pharmacokinetic parameters of Metronidazole were not affected by single dose administration of juice, on the other hand, multiple dose pre-treatment with juice significantly elevating the maximum plasma concentration (C-max) (PË‚0.05) and the area under the curve (AUC) of Metronidazole (P=0.001). Since there was a very slight changing on the t½ and the elimination rate constant, the hepatic enzymes could not be affected. In contrast, concomitant administration of Metronidazole and Clarithromycin showed no significant interaction.

Since there are different enteric metabolic enzymes involved in the orally administered drug metabolism, further in vitro and in vivo investigations to study the mechanism of the pomegranate juice effect on the pharmacokinetic parameters of these drugs should be established.

Biography:

Faiza Diaba studied chemistry at the University of Constantine, Algeria. She then obtained her Ph.D. in organic chemistry with Dr. Micheline Grignon-Dubois at Bordeaux I University, France. After a two years postdoctoral position with Prof. Josep Bonjoch at Barcelona University she pursued her scientific career as a lecturer then since 2009 she has been an associate professor at the same University. Her research interests are focused on developing new accessible synthetic methodologies for the synthesis of nitrogen-containing heterocycles directed to the total synthesis of natural compounds using radical chemistry, organocatalysis and electrophilic cyclizations promoted by NIS.

Abstract:

Daphniphyllum alkaloids, isolated from the Daphniphyllum genus, are a large family of natural compounds containing over than 320 members with more than 20 different polycyclic frameworks.Besides their fascinating structures, many of these compounds have showed a wide range of biological activities naming anticancer, anti-HIV, antioxidant, antiviral, vasorelaxation and nerve growth factor-regulation.Daphenylline, isolated in 2009 from the fruit of D. longeracemosum by Hao and co-workers, is the first member of the Daphniphyllum alkaloids including a benzene ring in the core structure.³ Since its isolation, four total syntheses of daphenylline⁴ and three other approximations to either the ABCE or the ACDE tetracyclic structures⁵ were reported. In this investigation we achieved the synthesis of the ACDEF pentacyclic structure of daphenylline from 1-methyl-2-tetralone as a starting material. The synthesis started with the preparation of enamide 1 which underwent a 5-endo-trig radical cyclization in the presence of Bu₃SnH and AIBN⁶ to provide indol 2 with all-carbon quaternary centers present in Daphenylline. Next, a stereocontrolled allylation followed by a diastereoselective reduction of the resulting enamide with NaBH₃CN and acetic acid gave 3 embedding the cis-hydroindole structure. Alkene 3 was converted to the corresponding acid using a two steps sequence: i) hydroboration-oxidation, ii) oxidation in the presence of TEMPO and NaClO. The acid was treated with SOCl₂ and then submitted to the classical Friedel-Crafts conditions to provide the seven-membered ring in 4 with an excellent yield.  After a 1,2-carbonyl transposition of ketone 4 using a four steps sequence, alkylation provided ester 5 with the correct stereochemistry which after a second friedel Crafts cyclization gave 6 with the ACDEF pentacyclic core of daphenylline.

Biography:

Pranjal Kalita is working as Associate Professor in the Department of Chemistry at Central Institute of Technology (CIT), Kokrajhar, Assam, India. His research areas are heterogeneous catalysts, pyrolysis, alternative fuels and chemicals. He has obtained his PhD at National Chemical Laboratory, Pune (India) in 2008. Prior to joining CIT, TERI, he has spent professional time in TERI, New Delhi and a five years of postdoctoral research including National Institute for Materials Science, Tsukuba, Japan; Iowa State University & Georgia Institute of Technology, USA. Currently, he is devoting his time in the utilization of biomass as heterogeneous catalyst and porous heterogeneous catalyst for synthesis of chemical intermediate and value-added products.

Abstract:

Bio-wastes materials are the post-harvest products, created by several agricultural activities in diverse scopes in various sectors. Efficient utilization of bio-waste is purely environmental benign system and cost-effective process of waste management and holds major challenges in sustainable human society nowadays. Among the different species of banana, Bhimkol/Aathiakol scientifically named as Musa balbisiana Colla is most commonly available in North-Eastern region of India. The ash obtained from the filtrate of the extract of ash and water is called Kolakhar. The analytical result confirmed the presence of K₂O with 25.09%”. Using Kolakhar, several traditional dishes are available in Assam, and it replaces the commercially available soda. This indicates that Kolakhar is a basic liquid, and has a wide scope as bio-waste catalyst for various applications especially base-catalyzed biodiesel synthesis and ligand free Suzuki–Miyaura Cross-Coupling reaction. Because of the high basicity of Kolakhar, we are expecting successive aldol condensation of 5-hydroxymethylfurfuraldehyde/furfuraldehyde with acetone that produces jet fuel intermediate chemicals. The yield of the desired product was around 95%. Among waste derived lignocellulose has been considered for the sources of platform chemicals such as 5-hydroxymethylfurfuraldehyde and furfural and fuels with value-added compounds due to easy availability and nonedible property. The cellulosic and hemicellulosic biomass could be converted into hexose and pentose sugars by acid hydrolysis process. Although, it is an important potential source for chemical intermediates, suitable traditional technology is being sought. Thus, we have reported for the conversion of waste biomass derived C6 and C5 (fructose and xylose) to platform chemicals, respectively, using super acid functionalized porous heterogeneous catalysts with yield around found to be 96%. Both the works provide a new technology for minimization of waste material to applicable material as well as its impact on reducing GHG emission and climate change.