Preface

2007 ◽  
Vol 79 (2) ◽  
pp. iv
Author(s):  
Guillermo Delgado

Organic synthesis continues to grow and develop impressively in response to new research challenges at the boundaries of structural complexity, while playing a central role in the industrial activities and applications of the chemical sciences. The International Conferences on Organic Synthesis (ICOS), which have been organized biennially around the world since 1976 under IUPAC sponsorship, faithfully reflect this growth and development.The 16th event in this series (ICOS-16) was held in Mérida, México, from 11 to 15 June 2006. The scientific program included 22 plenary and invited speakers, as well as 36 experts who participated in symposia on medicinal chemistry, organocatalysis, enantioselective synthesis of β-amino acids, organolithium compounds in organic synthesis, organic selenium and tellurium compounds in organic synthesis, and applications of microwaves in organic synthesis. In addition, almost 300 posters covering all aspects of modern organic synthesis were displayed by scientists and research scholars. The strong Latin American participation in this feature of the program, followed by those of European, North American, and Asian delegates, attested to the growing contribution of this region to chemical research in organic synthesis. Overall, the scientific program offered comprehensive and fruitful coverage of organic synthesis from a variety of different perspectives.The Mexican Academy of Sciences and the Mexican Chemical Society (celebrating its 50th Anniversary) featured as cosponsors of ICOS-16 together with IUPAC. This was the second occasion that an IUPAC-sponsored conference has been held in Mexico, the first being the 6th International Symposium on Natural Products Chemistry in Mexico City, in 1969. ICOS-16 attracted almost 500 delegates from 40 countries, mainly those of Latin America, a gratifyingly high proportion of whom were younger scientists.This issue of Pure and Applied Chemistry contains a representative selection of papers based upon lectures delivered at ICOS-16. The theme of synthesis of natural products was covered by M. Brimble (New Zealand), L. C. Dias (Brazil), and C. Gennari (Italy). Different aspects on methodology and control of chemical reactivity were presented by J. Tamariz (Mexico), S. F. Martin (USA), S. Ma (China), and Ph. Renaud (Switzerland). Organic synthesis using phosphorous was covered by R. Réau (France) and C. Nájera (Spain). The broad topic of catalysis was presented by S. Kobayashi (Japan) and C. Crudden (USA). New insights on synthesis using epoxides and aziridines were disclosed by D. Hodgson (UK) and F. McDonald (USA).Organic synthesis is a fascinating field of chemistry that has often been compared with art. The control of regio-, stereo-, and site selectivity demands deep insight into chemical reactivity as well as knowledge of new and old methodology and catalysis, and the ability to combine these creatively in sustainable processes in order to achieve specific objectives. Despite remarkable progress during recent years, efficient synthesis of specific organic compounds with tailored activities and properties will continue to challenge future generations of chemists. Further progress of organic synthesis will be covered during the next conference in this series (ICOS-17), which will take place in Korea during 2008.Thanks are due to members of the ICOS-16 Committees, to all participants, and to authors contributing to this issue.Guillermo DelgadoConference Editor

2009 ◽  
Vol 81 (2) ◽  
pp. iv
Author(s):  
Sang-gi Lee

The 17th International Conference on Organic Synthesis (ICOS 17) was held in Daejeon, Korea during 22-27 June 2008 under the joint chairmanship of Prof. Eun Lee (Seoul National University) and Prof. Sunggak Kim (Korean Advanced Institute of Science and Technology). Professor Sung Ho Kang (Korean Advanced Institute of Science and Technology) acted as Chair of the Organizing Committee for the event, which is the latest in a regular biennial series that was initiated in 1974 under the auspices of IUPAC. On this occasion, the Korean Chemical Society acted as cosponsors, and the Conference enjoyed generous financial support from the Korean Research Foundation, the Korean Federation of Science and Technology Societies, and a sponsorship club representing Korean industries.Almost 1000 participants, including 412 foreign scientists, attended from 32 countries, once again demonstrating the ongoing international appeal and topicality of organic synthesis. The scientific program of ICOS 17 was characterized by in-depth coverage of many familiar aspects of the topic, such as synthetic methodology, natural products synthesis, bioorganic chemistry, chemical biology, organic materials, and medicinal chemistry. The program was delineated in five broad themes entitled:- Discovery of new reagents and reactions- Challenges and new trends in natural products synthesis- Prospects in bioorganic chemistry and chemical biology- Visions in organic materials researches- Events in drug discovery and process developmentA total of 51 invited lectures were delivered; in addition to 36 from academia, 13 emanated from industry and 2 from research institutes. A highlight of the lecture program was the Thieme-IUPAC prize lecture presented by Prof. Dean Toste (University of California, Berkeley, USA). The poster program was particularly well supported, and no less than 533 posters were presented during two sessions.This issue of Pure and Applied Chemistry comprises a collection of 12 papers based on lectures delivered at ICOS 17. The organizers are particularly grateful to all who contributed to this issue for their timely efforts. The topics of these papers feature some of the major themes of the conference and thus furnish a representative insight into the scientific program and capture exciting new developments and trends. This series will continue in Bergen, Norway on 2-5 August 2010, and it is confidently expected that it will continue to fulfill an important scientific role in highlighting ongoing advances in modern organic synthesis.Sang-gi LeeConference Editor


Synthesis ◽  
2018 ◽  
Vol 51 (06) ◽  
pp. 1342-1352 ◽  
Author(s):  
Javier Izquierdo ◽  
Atul Jain ◽  
Sarki Abdulkadir ◽  
Gary Schiltz

The chromenone core is an ubiquitous group in biologically active natural products and has been extensively used in organic synthesis. Fluorine-derived compounds, including those with a trifluoromethyl group (CF3), have shown enhanced biological activities in numerous pharmaceuticals compared with their non-fluorinated analogues. 2-Trifluoromethylchromenones can be readily functionalized at the 8- and 7-positions, providing chromenones cores of high structural complexity, which are excellent precursors for numerous trifluoromethyl heterocycles.


2022 ◽  
Vol 13 (1) ◽  
Author(s):  
Masaya Nakajima ◽  
Yusuke Adachi ◽  
Tetsuhiro Nemoto

AbstractAlthough computational simulation-based natural product syntheses are in their initial stages of development, this concept can potentially become an indispensable resource in the field of organic synthesis. Herein we report the asymmetric total syntheses of several resveratrol dimers based on a comprehensive computational simulation of their biosynthetic pathways. Density functional theory (DFT) calculations suggested inconsistencies in the biosynthesis of vaticahainol A and B that predicted the requirement of structural corrections of these natural products. According to the computational predictions, total syntheses were examined and the correct structures of vaticahainol A and B were confirmed. The established synthetic route was applied to the asymmetric total synthesis of (−)-malibatol A, (−)-vaticahainol B, (+)-vaticahainol A, (+)-vaticahainol C, and (−)-albiraminol B, which provided new insight into the biosynthetic pathway of resveratrol dimers. This study demonstrated that computation-guided organic synthesis can be a powerful strategy to advance the chemical research of natural products.


2005 ◽  
Vol 77 (7) ◽  
pp. iv
Author(s):  
Tamejiro Hiyama

Organic synthesis has long played a pivotal role in the chemical sciences. It is therefore unsurprising and appropriate that the International Conferences on Organic Synthesis (ICOS) continue to thrive. This series was initiated by IUPAC in 1976 and has since featured biennially as one of the core events of the Union. What is surprising is that 22 years have elapsed since an ICOS event was last hosted by Japan. On that occasion, ICOS-4 was held in 1982 at Shinjuku, Tokyo, and was acclaimed as a great success. The latest event (ICOS-15), in Nagoya, Japan on 1ñ6 August 2004, offered an opportunity to match or surpass the impact of its predecessoróa challenge that was taken up enthusiastically under the leadership of Profs. Minoru Isobe (Nagoya University) and Hisashi Yamamoto (now at the University of Chicago) as Conference co-Chairs. Almost 1000 participants converged on Nagoya from all parts of the world. A noticeably high level of participation by delegates from East Asia in relation to those from North America and Europe attested to the growing capacity of this region to contribute to research at the forefront of this area of the chemical sciences. The scientific program of the Conference embraced all aspects of modern synthetic organic chemistry, inter alia, the invention of selective synthetic methods, asymmetric synthesis, total synthesis of natural products, design and synthesis of artificial agents for pharmaceutical and agricultural uses, and molecular assembly and materials based on molecular function. This topical breadth was also captured in a poster program, which was handsomely supported by no less than 466 displays on every conceivable facet of the subject. Overall, it is evident that organic synthesis has expanded its boundaries increasingly toward biological and material sciences, in response to the new challenges arising from rapid progress in molecular biology and applied physics during recent years.A lecture program comprising 10 plenary and 20 invited presentations, in addition to the Thieme/IUPAC award lecture and two Nagoya medal lectures, contributed to a truly exciting Conference experience, and the 21 speakers who kindly agreed to contribute papers based upon their presentations have made it possible to capture some of the excitement in this issue of Pure and Applied Chemistry. The Nagoya Gold Medallist, J. F. Stoddart, used the occasion to share an absorbing and very personal perspective on molecular assembly and materials, a theme on which M. Fujita also disclosed new insights and developments. The perennial theme of total synthesis of natural products, provided scope for presentation of highly creative accomplishments by S. Ley, J. Cossy, Y. Langlois, R. Pilli, and S. Kozmin on a variety of challenging targets. Such advances in the total synthesis of biologically active natural products having extremely complex structures, often necessitate development of novel synthetic methods, and H. Overkleeft, P. Chiu, V. Nair, T.-P. Loh, S. Martin, T.-Y. Luh, E. Juaristi, and M. Catellani did justice to this theme with presentations on a variety of extremely elegant and sophisticated new developments in methodology, based upon organometallic catalysts and/or reagents. Finally, the broad theme of asymmetric synthesis using organometallic complexes with chiral ligands or chiral organocatalysts was developed in conjunction with combinatorial methodology, which is shown to be highly effective in optimizing catalytic systems. Those who contributed to the topic of asymmetric synthesis are K. Ding, A. Charette, S. H. Kang, A. Berkessel, and K. Maruoka, the recipient of the Nagoya Silver Medal.What is the future of organic synthesis? The invention of unprecedented drugs and materials has enriched and expanded the horizons of the human experience in formerly unimagined ways, and owes much to the ever increasing ingenuity of organic synthesis, and recognition and attainment of new synthetic targets. The impact of organic synthesis on cognate disciplines and on general advancement of science and technology is definitely enormous and will be further strengthened by future challenges and opportunities. Thus, it is hoped that younger generations will be inspired to participate in tapping this rich potential, in the cause of advancing science and contributing to the enrichment of future life. These aspirations may yield incalculable rewards. Such progress will certainly be reflected in the scientific program of the next Conference in the ICOS series, which will take place in Merida, Yucatan, Mexico on 11ñ15 June 2006, under the chairmanship of Dr. Eusebio Juaristi, Instituto Politecnico Nacional, Mexico.Tamejiro HiyamaConference EditorDepartment of Material ChemistryKyoto University, Kyoto, Japan *An issue of reviews and research papers based on lectures presented at the 15th International Conference on Organic Synthesis (ICOS-15), held in Nagoya, Japan, 1-6 August 2004, on the theme of organic synthesis. Other presentations are published in this issue, pp. 1087-1296.


2010 ◽  
Vol 82 (9) ◽  
pp. iv
Author(s):  
Paris E. Georghiou

The 22nd International Congress on Heterocyclic Chemistry (ICHC-22) was held 2-7 August 2009 in St. John's, Newfoundland and Labrador, Canada. St. John's, the capital of Canada's youngest Province, Newfoundland and Labrador, is also Canada’s oldest and North America’s most easterly city. The Conference was chaired by Prof. Mohsen Daneshtalab (School of Pharmacy, Memorial University of Newfoundland) and was organized by the School of Pharmacy and the Chemistry Department at Memorial University of Newfoundland.Approximately 260 participants from over 30 different countries attended. The scientific program consisted of 10 plenary lectures, 19 invited lectures, 52 short communications, and 115 posters. Prof. Samuel Danishefsky (Sloan-Kettering Institute for Cancer Research, Columbia University) was honored with the 2009 ISHC Senior Award in Heterocyclic Chemistry, and Prof. John Wood (Colorado State University) was the 2009 Katritzky Junior Award winner. A special symposium entitled "Focus on heterocycles in organic synthesis today and tomorrow" was held during the Congress as a tribute to Prof. Victor Snieckus (Queen's University, Kingston) for his research accomplishments and long-time contribution to the International Society of Heterocyclic Chemistry (ISHC).The five Congress themes were:- New Methods in Heterocyclic Chemistry- Biologically Active Heterocycles (Pharmaceuticals/Agrochemicals)- Heterocyclic Natural Products and their Analogues- Applications of Heterocycles in Organic Synthesis- Heterocycles in Materials ScienceBesides the collection of 9 papers that are based on the plenary and invited lectures included in this issue of Pure and Applied Chemistry, the ICHC-22 Book of Abstracts is available online and can be downloaded for free from http://www.ichc2009.ca/abstract_book.pdf in pdf format.ICHC-23 will be held in Glasgow, Scotland, 31 July to 5 August 2011 with the following five main themes of heterocyclic chemistry: synthetic methodology, natural products and complex molecule synthesis, materials, medicinal chemistry, and nanochemistry. The conference will be chaired by Prof. Colin Suckling (University of Strathclyde).The organizers are grateful to all who contributed to a successful scientific program, especially to the speakers and to our public and private sponsors: City of St. John's, Memorial University of Newfoundland, IUPAC, Thieme, Wiley-Blackwell, Elsevier, Taiho Pharmaceutical Co., ChemRoutres Corporation, and American Diagnostica, Inc.Paris E. GeorghiouConference Editor


2018 ◽  
Vol 15 (2) ◽  
pp. 221-229 ◽  
Author(s):  
Shah Bakhtiar Nasir ◽  
Noorsaadah Abd Rahman ◽  
Chin Fei Chee

Background: The Diels-Alder reaction has been widely utilised in the syntheses of biologically important natural products over the years and continues to greatly impact modern synthetic methodology. Recent discovery of chiral organocatalysts, auxiliaries and ligands in organic synthesis has paved the way for their application in Diels-Alder chemistry with the goal to improve efficiency as well as stereochemistry. Objective: The review focuses on asymmetric syntheses of flavonoid Diels-Alder natural products that utilize chiral ligand-Lewis acid complexes through various illustrative examples. Conclusion: It is clear from the review that a significant amount of research has been done investigating various types of catalysts and chiral ligand-Lewis acid complexes for the enantioselective synthesis of flavonoid Diels-Alder natural products. The results have demonstrated improved yield and enantioselectivity. Much emphasis has been placed on the synthesis but important mechanistic work aimed at understanding the enantioselectivity has also been discussed.


Author(s):  
Mengyu Qiu ◽  
Xuegang Fu ◽  
Peng Fu ◽  
Jianhui Huang

N-heterocycles can be found in natural products and drug molecules, which are indispensable components in the area of organic synthesis, medicinal chemistry and material science. The construction of these N-containing...


1988 ◽  
pp. 343-359 ◽  
Author(s):  
Johann Gasteiger ◽  
Michael G Hutchings ◽  
Heinz Saller ◽  
Peter Löw

Author(s):  
Beatriz de las Heras Polo

Natural products have historically contributed to drug discovery as a source of bioactive molecules, due to their great diversity and structural complexity. They have provided “lead” molecules for the development of drugs in different therapeutic areas, with a very prominent representation in the treatment of pain and inflammation, coagulation disorders, metabolic disorders, as well as in the treatment of cancer and infectious diseases. In recent decades there has been a paradigm shift in drug discovery strategies that has allowed the identification of new active natural products in therapeutic targets. Combinatorial Chemistry and biological tests (High Throughput Screening), together with the development of computational techniques, have contributed decisively to the design and optimization of libraries of natural product derivatives based on their biological activity. In parallel, technological advances in the field of Omics sciences and in data processing lead to a multidimensional approach in the drug discovery process. These powerful tools will allow the analysis of the pharmacological potential of natural products and their derivatives for the conversion of these molecules to active products with low toxicity. In the Precision Medicine era, natural products continue to be molecules with great potential in pharmaceutical development, since, unlike other therapeutic strategies, they have a favorable cost-benefit ratio, which will allow their future use in this discipline.


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