微波合成加速有固相协助的液相反应

2006-08-03 22:23  下载量:308

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Solid-Assisted Solution Phase Synthesis (SASPS) is a technique where the target molecule is synthesized in solution and solid-supported molecules are used as reagents, catalysts or scavengers. Recently this technique has been getting a lot of attention as an alternative to solid phase organic synthesis (SPOS), since it offers many of the advantages of SPOS in terms of ease of reaction workup and product purification in addition to the advantages associated with traditional solution-phase chemistry (e.g. the ease of monitoring the progress of the reaction by simply applying LC-MS or TLC techniques). A disadvantage of this technique is the relative slow reaction rate, and many of these reactions are sluggish and require hours for complete conversion. The advent of Microwave-Assisted Organic Synthesis (MAOS) has helped accelerate these reactions and the technique is gaining rapid popularity as evidenced by the increasing number of publications on this topic. The polymer backbones are in general, stable at the high temperatures used with MAOS for the short periods of time required for most of these reactions. This technique is particularly well-suited for automation and can easily incorporate in-line purification protocols, such as reagent and byproduct scavenging and catch-and-release. This introduces the possibility of direct highthroughput synthesis of compounds with intrinsically high purities suitable for biological screening without the need for further purification.

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