SYNFORM is available as part of the online editions of SYNTHESIS, SYNLETT and SYNFACTS through Thieme eJournals. This supplementary feature is available free of charge. SYNFORM presents people, trends, and views in synthetic organic chemistry with direct links to all quoted original papers. To view or download issues of SYNFORM, please click here.
The importance of organic synthesis is dramatically growing in biomedical research, as scientists are making great progress in understanding biomedical processes at molecular level and are learning how to rationally exploit these molecular processes for diagnostic and therapeutic purposes. There is little doubt that one particular area of research where chemistry is playing a pivotal role, right at the center of the innovation process, is in the field of imaging, where the emphasis is currently all placed on the discovery of novel tracers and molecular systems for clinical applications. Organic and synthetic chemists are increasingly working in multidisciplinary teams of researchers, side by side with biologists, physicists, engineers and medical doctors. This exciting trend is well exemplified by the first SYNSTORY of this issue, which reports on a truly brilliant chemistry-driven piece of research developed by a highly interdisciplinary team at Philips Research (The Netherlands) that led to the identification of an in vivo reaction allowing for an efficient tumor imaging in live mice. In my humble opinion, this is one of the most exciting recent achievements in the area of molecular imaging, which opens up whole new perspectives in molecular biomedicine. The second SYNSTORY reports on another exciting work dealing with a very timely area of research where organic chemistry obviously occupies a central role: catalysis and environmental sciences. Pressure is mounting on chemists to identify more environmentally compatible, sustainable and green chemical processes, and the work recently published by Professor K. Ishihara (Japan) goes in the right direction as, besides being a fantastic scientific contribution, it might help identifying more efficient organic catalysts for oxidation reactions, as an alternative for the more toxic metal catalysts. The issue is completed by a brief report on a very well organized and truly international School of Medicinal Chemistry for postgraduate researchers, the ESMEC, which is held annually in Urbino (Italy).
The field of bioconjugates, and more specifically that of bioorthogonal chemistry, has rapidly expanded over the last few years, and the sequential discovery of more effective reactions has unearthed a wealth of exciting new possibilities for probing and perturbing biological systems. The exquisite selectivity of these reactions has been successfully exploited for biomolecule modifications in complex environments such as live cells. “However,” pointed out Dr. Marc S. Robillard, from the Biomolecular Engineering group of Philips Research in Eindhoven (The Netherlands), “these reactions have only in a few cases been successfully used in living organisms.”
To read more please download SYNFORM 2010/09 online, free of charge.
Organocatalysis is a very hot area of research and a number of acid and base organocatalysts have been developed recently. In contrast, there are only a few known organic redox catalysts. “I am convinced that hypervalent halogen compounds will soon become competitive with transition-metal redox catalysts,” said Professor Kazuaki Ishihara from Nagoya University (Japan).
To read more please download SYNFORM 2010/09 online, free of charge.
From July 4th to 9th, 2010, Urbino (Italy) hosted the European School of Medicinal Chemistry. The venue was the Scientific Campus of the University of Urbino, located on a hill at about 3 km from the historical city center of Urbino, with its charming view of the surrounding countryside. The school was attended by 196 young scientists, 170 of them being PhD students, from 10 different European countries.
To read more please download SYNFORM 2010/09 online, free of charge.
It’s a real pleasure to write this brief editorial while quietly travelling on a train in the beautiful Italian country - side between Pesaro and Bologna. I had a delightful breakfast this morning with a cappuccino and a hot croissant, and I feel really peaceful now. To be honest, there is railway strike today and I am not quite sure how I will be able to continue my travel after Milan, but that’s part of the pleasures and pains of being in Italy. In the worst case I will just wait for the next train in a restaurant, enjoying a good pizza. Or even two, if the next train will be really late... Once again, I realize I am writing about food, so let’s switch to the real topic: good chemistry, as usual. The first SYNSTORY of this issue is about a novel multicomponent reaction leading to phosphonyl pyrazoles, developed by M. Smietana and J.-J. Vasseur (France). The second covers a novel amination reaction of heteroaromatic C–H bonds, as reported by M. Miura (Japan). The issue is closed by a short report on the last Thieme Chemistry Journals Editorial Board Meeting 2010 in Florence (Italy). Meanwhile I am just arrived at the Central Railway Station of Milan. The departures’ big screen is desolately empty. I am afraid I will have to make plans for dinner too...
No one who has given even a passing glance to the literature of organic chemistry will have failed to note a flourishing development of step-economic reactions that achieve multiple bond formations in one operation. In this context, multicomponent reaction (MCR) processes usually satisfy most criteria (readily available starting reagents, atom-economical, environ - mentally friendly, etc.) required for ideal organic syntheses. Undoubtedly, such reactions offer an efficient way to generate complex molecular frameworks due to their inherent convergence and complexity-generating ability.
To read more please download SYNFORM 2010/08 online, free of charge.
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Over the last decade, transition-metal-mediated or -catalyzed reactions involving a C–H bond cleavage have received much attention and the area has grown rapidly because of the possibility of transforming ubiquitous C–H bonds into versatile functions in just one synthetic step. In 1997, Professor Masahiro Miura and co-workers from Osaka University (Japan) reported the palladium-catalyzed direct arylation of phenolic compounds with aryl halides (Angew. Chem., Int. Ed. Engl. 1997, 36, 1740), which is one of the pioneering works in the field of C–H bond activation chemistry.
To read more please download SYNFORM 2010/08 online, free of charge.
The 2010 Editorial Boards Meeting of the Thieme Chemistry journalsSYNLETT, SYNTHESIS and SYNFACTS, including the supplement SYNFORM, took place on 21st and 22nd of May 2010 in the city of Florence (Italy). The Editorial Boards of the three journals and the staff of the Thieme Chemistry editorial office met at the Grand Hotel Villa Medici. A great deal of attention was devoted to the current difficult global financial and economic situation that, not surprisingly, is also having an impact on the world of scientific publishing.
To read more please download SYNFORM 2010/08 online, free of charge.
There is little doubt that these are difficult days for scientific research, which is stuck between a rock and a hard place. Indeed, most universities and research institutions are cutting research budgets in an attempt to save money and limit redundancies, whereas costs of research are increasingly growing. This exercise of remaining competitive with reduced budgets requires remarkable creativity both from scientists and research managers, but every cloud has a silver lining and these hard times might eventually help to streamline and optimize the research output and organization of many research institutions. In terms of creativity, the protagonists of this issue of SYNFORM are absolute leaders. Abigail G. Doyle (USA) has developed an intelligent strategy to circumvent the inherently low reactivity and organic solubility of the fluoride anion, using benzoyl fluoride in an enantioselective epoxide ring-opening reaction. Hisashi Yamamoto (USA) has developed a highly 1,3-syn-selective aldol reaction methodology exploiting the potential of superbulky silyl protecting groups. Great creativity, great results! The issue is completed by a brief profile of Lutz Ackermann (Germany), Editorial Advisory Board member of SYNLETT and SYNTHESIS.
Stereocontrolled incorporation of fluorine into organic molecules remains a challenging endeavor, despite remarkable recent progress in the field. The use of fluoride anion in catalytic C–F bond-forming reactions is particularly attractive, not only for economic and environmental reasons, but also because it could have important applications in emerging fields, such as positron emission tomography. Recently, the group of Professor Abigail G. Doyle from Princeton University (USA) reported an interesting methodology for the ring opening of meso-epoxides by fluoride anion.
To read more please download SYNFORM 2010/07 online, free of charge.