Fluorine substitution is an established tool in medicinal chemistry to favourably alter the molecular properties of a lead compound of interest. However, gaps still exist in the library of synthetic methods for accessing certain fluorine-substituted motifs. One such area is the fluoromethyl group, particularly when required in a fluoroalkylating capacity. The cold fluorination of methylene ditosylate is under evaluated in the literature, often proceeding with low yields or harsh conditions. This report describes a novel microwave method for the rapid nucleophilic fluorination of methylene ditosylate using inexpensive reagents in good isolated yield (65%).

氟取代是药物化学中已建立的工具，可以有利地改变目标铅化合物的分子性质。但是，在合成方法的文库中仍然存在缺口，以获取某些氟取代的基序。一种这样的区域是氟甲基，特别是在需要氟烷基化能力时。对二甲苯磺酸甲酯的冷氟化在文献中进行了评估，通常以低收率或苛刻的条件进行。该报告介绍了一种新型的微波方法，该方法使用廉价的试剂以良好的分离产率（65％）对二甲苯磺酸亚甲基酯进行快速亲核氟化。