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Proteeting-Group-Free Total Syntheses: A Challenging Approach

机译:无团体自由的全面综合:具有挑战性的方法

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Multistep synthesis, and in particular, total synthesis of natural product is a refined scientific activity. After two centuries of breakthroughs, organic chemistry has become a "predictive science" just as, for example, nuclear physic. However, total synthesis remains an activity so difficult that designing a totally reliable relrosynthctic plan remains almost impossible. Over many decades, the objectives of total synthesis were solely to get higher yields, higher chemo- and stereoselectivity, and higher convergence. Nevertheless, this led to much innovative success. In the mid 90s, a new philosophy arose for multistep synthesis that took new constrains into account: step economy, atom economy, and redox economy. This put stimulating pressure on chemists' inventiveness and led to even more aesthetic and straightforward syntheses. Pushed forward by the demands of our society, chemical science must now go one more step toward maturity by taking into account ecologic considerations. This means that chemists must now design retrosynthetic plans incorporating protective-group-free strategies, thus adding a further refinement to the already complicated art of total synthesis. Thanks to tremendous advances recently accomplished in organic chemistry, and particularly in catalyzed processes, this refinement is now a reachable aim. Thus, many new kinds of catalyst are now described, and they are endowed with always higher selectivity, functional group tolerance, thus allowing milder conditions and accomplishing ewactions hitherto unprecedented. Chemistry catalogues list many of them, and these catalysts involve almost all the elements of the periodic table.
机译:多步合成,特别是天然产物的全合成是一种精细的科学活动。经过两个世纪的突破,有机化学已成为“预测科学”,就像核物理一样。然而,全合成仍然是一项艰巨的任务,以至于设计一个完全可靠的相关合成计划几乎是不可能的。几十年来,全合成的目标仅仅是获得更高的产量,更高的化学和立体选择性以及更高的收敛性。尽管如此,这还是取得了很大的创新成功。在90年代中期,出现了一种新的多步合成哲学,其中考虑了新的约束条件:步进经济,原子经济和氧化还原经济。这给化学家的发明创造施加了巨大压力,并导致了更加美观和直接的合成。在我们社会的要求推动下,化学科学现在必须考虑到生态因素,向成熟迈出又一步。这意味着化学家现在必须设计结合了无保护基团策略的逆合成计划,从而进一步完善了已经复杂的全合成技术。得益于有机化学,特别是催化工艺领域最近取得的巨大进步,这种改进现已成为可实现的目标。因此,现在描述了许多新型催化剂,并且它们始终具有更高的选择性和官能团耐受性,从而允许较温和的条件并完成迄今为止前所未有的反应。化学目录中列出了许多,这些催化剂几乎涉及元素周期表中的所有元素。

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