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A short and efficient synthesis of 3-{2-[2-(bromomethyl)thiazol-4-yl]ethynyl}-5-fluorobenzonitrile:
A precursor for PET radioligand [F-18]SP203
Gopinathan, M., Jin, C., & Rehder, K. (2009). A short and efficient synthesis of 3-{2-[2-(bromomethyl)thiazol-4-yl]ethynyl}-5-fluorobenzonitrile: A precursor for PET radioligand [F-18]SP203. Synthesis, 2009(12), 1979-1982. https://doi.org/10.1055/s-0029-1216787
An improved synthesis of 3-{2-[2-(bromomethyl)thiazol-4-yl]ethynyl}-5-fluorobenzonitrile, a precursor for PET radioligand [¹8F]SP203, is described, wherein a new synthon was employed for Sonogashira coupling with 3-bromo-5-fluorobenzonitrile. The new five-step synthesis provided the title compound in 56% overall yield starting from 4-bromo-2-formylthiazole.