A Short and Efficient Synthesis of 3-{2-[2-(Bromomethyl)thiazol-4-yl]-ethynyl}-5-fluorobenzonitrile: A Precursor for PET Radioligand [18F]SP203

doi:10.1055/S-0029-1216787

Paper

A Short and Efficient Synthesis of 3-{2-[2-(Bromomethyl)thiazol-4-yl]-ethynyl}-5-fluorobenzonitrile: A Precursor for PET Radioligand [18F]SP203

Published May 31, 2009 · M. Gopinathan, Chunyang Jin, K. Rehder

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Abstract

An improved synthesis of 3-{2-[2-(bromomethyl)thiazol-4-yl]ethynyl}-5-fluorobenzonitrile, a precursor for PET radioligand [ 18 F]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.

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The improved synthesis of 3-2-[2-(bromomethyl)thiazol-4-yl]-ethynyl-5-fluorobenzonitrile, a precursor for PET radioligand [18F]SP203, provides a 56% overall yield from 4-bromo-2-

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

A Short and Efficient Synthesis of 3-{2-[2-(Bromomethyl)thiazol-4-yl]-ethynyl}-5-fluorobenzonitrile: A Precursor for PET Radioligand [18F]SP203

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References

Citations

Synthesis and characterization in monkey of [11C]SP203 as a radioligand for imaging brain metabotropic glutamate 5 receptors

[11C]SP203 provides a large mGluR5-specific signal in monkey brain, but is unstable in monkey blood and unsuitable for quantification in monkey brain.