Process research and development of a dihydropyrimidine dehydrogenase inactivator: Large-scale preparation of eniluracil using a Sonogashira coupling

…, R Bright, MJ Coleman, KP Jenkins

文献索引：Cooke, Jason W. B.; Bright, Robert; Coleman, Mark J.; Jenkins, Kevin P. Organic Process Research and Development, 2001 , vol. 5, # 4 p. 383 - 386

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被引用次数: 49

摘要

Eniluracil (5-ethynyluracil) is a potent inactivator of the enzyme dihydropyrimidine dehydrogenase, which is the rate-limiting enzyme in the metabolism of 5-fluorouracil, a widely used anti-cancer drug. The process research and development of a three-stage route to eniluracil is described. A Sonogashira coupling between 5-iodouracil and trimethylsilylacetylene was used to synthesise 5-(2-trimethylsilylethynyl) uracil on a> 60 kg ...