期刊
JOURNAL OF FLOW CHEMISTRY
卷 3, 期 2, 页码 46-50出版社
SPRINGER
DOI: 10.1556/JFC-D-13-00004
关键词
flow chemistry; microfluidics; fluorine; positron emission tomography; Sonogashira coupling
资金
- Department of Energy [DE-SC0001781]
- U.S. Department of Energy (DOE) [DE-SC0001781] Funding Source: U.S. Department of Energy (DOE)
Continuous-flow methodologies have been applied to the synthesis of a number of fluorinated alkynyl arenes and heteroarenes. Through a series of optimizations reagent stoichiometry and reaction time were improved and substrate specificity was interrogated. Using optimized conditions under copper-free Sonogashira type couplings readily available arene building blocks were derivatized with fluoroalkynyl side chains in <10 min. Given the rapidity of the process and the enhanced purity profile of the products an immediate application of the work is in the development of F-18 labeled versions of the agents for subsequent use in positron emission tomography (PET) imaging. A homolog of the Alzheimer's disease imaging agent Fallypride (R) was prepared using the methodology and additional analogs was identified.
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