是否存在合理化学合成的极限?  

Are there limits to rational chemical synthesis?

作　　者：许正双[1] 叶涛[1] XU ZhengShuang YE Tao(School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, China)

机构地区：[1]北京大学深圳研究生院化学生物学与生物技术学院,深圳518055

出　　处：《科学通报》2017年第21期2313-2322,共10页Chinese Science Bulletin

摘　　要：合成化学作为古老的学科之一,曾经是自然科学的重要领域和支撑点.随着现代合成、分析和仪器的进步,特别是随着合成化学的不断发展及其在生物化学、材料化学等领域的应用不断深入,人们关心的重点已经从早期的合成目的逐渐过渡到更加贴近生活的应用领域.例如所合成的分子用于医疗和特殊材料领域时,人们看到的往往是这些分子表现出来的特性和作用,因为这更加直观,而其背后的分子基础和制备这些分子的艺术却在有意无意之间被逐渐淡化.另外,由于合成化学自身的发展促使各种新颖的方法学不断被开发出来,设计巧妙的原子经济、氧化还原经济、无保护基等策略的应用,使得针对特定分子的合成的相对难度在不断的降低,甚至有人认为"没有合成不了的分子".理性合成的化学学科似乎已经发展到了极限,然而真相究竟如何?究竟是否存在合理化学合成的极限?这是Science提出的125个科学前沿问题之一.本文试图从合理化学合成的历史、近期发展等角度探讨这一问题的内涵.Chemical synthesis is the purposeful execution of one or more reactions to obtain a product, or several products, which could modify the existing molecular frameworks, or make a complex（often natural） molecule from simple reagents. There are several possible reasons to make complex molecules by total chemical synthesis. A century ago the aim was often to identify a molecular structure. With the advent of routine X-ray crystallography and high-field FT NMR in the late 1960s, total chemical synthesis served as a necessary structural confirmation became much less compelling. Another reason that chemists synthesized natural products was because of their useful properties. In some cases, molecules could be cheaper to make from scratch than to obtain from nature source. The history of chemistry is essentially the history of finding out the structure of molecules and of developing new and efficient methods of making them. Putting these molecules to new uses is what underpins our modern world, but it was really a secondary goal for most of chemistry＇s history. Great synthetic chemists of the mid-to-late twentieth century are revered not so much for what they made but for how they made it. Synthesis cultivates an understanding of the basic principles of chemistry： how and why reactions occur, the relationships between molecular shape and function, and so on. Today, synthetic chemists still need to pursue ＂ideality＂ in the way molecules are synthesized, and total synthesis should be able to provide large quantities of complex natural products with a minimum amount of labor and material expense. In future years, the emphasis of synthetic chemistry, also natural product synthesis, will shift from delivering structures to delivering functions. Natural products will continue to serve a central role in the discovery and development of pharmaceutical agents as well as the elucidation of new biological targets of therapeutic relevance. Synthetic chemists are in a unique position to define those very important molecule

关 键 词：理性化学合成 全合成 理想合成 天然产物 药物发现 

分 类 号：O6[理学—化学]