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首页> 外文期刊>Journal of Chemical Education >Introducing Freshmen Students to the Practice of Solid-Phase Synthesis
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Introducing Freshmen Students to the Practice of Solid-Phase Synthesis

机译:向新生介绍固相合成的实践

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Solid-phase chemistry has revolutionized the synthesis of organic compounds, peptides, oligouncleotides, carbohydrates, drugs, and combinatorial libraries (1-5). Although many types of compounds incorporating a variety of building blocks can be created, all solid-phase syntheses share a common approach. In a typical synthesis, starting material is anchored to a polymeric support and transformed into product by the action of solution-phase reagents. The product is then liberated into solution. The reverse approach has been used to convert solution-phase reactions into products by means of support-immobilized reagents and catalysts (6). Solid-phase organic synthesis is effective because reagents can be used in excess to drive reactions and immobilized products can be purified by repeated washings (7). In addition, syntheses can be automated. By solid-phase protocols are illustrated by the example of Bruce Merrifield, who received a Nobel Prize for his seminal contribution, and further, by explosive developments in combinatorial chemistry and drug discovery (5,8-11).
机译:固相化学彻底改变了有机化合物,肽,寡核苷酸,碳水化合物,药物和组合库的合成方法(1-5)。尽管可以创建结合了多种结构单元的多种类型的化合物,但所有固相合成方法都具有相同的方法。在典型的合成中,原料通过溶液相试剂的作用固定在聚合物载体上并转化为产物。然后将产物释放到溶液中。反向方法已用于通过固定有载体的试剂和催化剂将溶液相反应转化为产物(6)。固相有机合成是有效的,因为可以过量使用试剂来驱动反应,并且固定的产物可以通过反复洗涤进行纯化(7)。另外,合成可以自动化。布鲁斯·梅里菲尔德(Bruce Merrifield)举例说明了固相方案,他因其开创性贡献而获得了诺贝尔奖,此外,组合化学和药物发现的爆炸性发展也获得了诺贝尔奖(5,8-11)。

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