Effect of leaving group substituents on the microfluidic synthesis of [18F]3-Fluoro-5-[(Pyridin- 3-YL)Ethynyl]benzonitrile ([18F]FPEB)

Thomas M. Moore, Murthy Akula, Lee Collier, Gilles Tamagnan, Caroline Papin, David Alagille, George Kabalka

Research output: Contribution to journalArticle

Abstract

A commercial microfluidic reactor system has been used to synthesize the mGLUR5 receptor imaging agent [18F]FPEB. To study the effect of leaving group substituents on the synthesis of the desired compound, the chloro-, bromo-, iodo-, and nitro-substituted precursors for FPEB were evaluated. Precursor concentrations of 4 - 10 mg/mL were evaluated in various solvents, with temperature ranges between 120 and 220 oC, and total processing times of less than five minutes. Optimized incorporation yields ranged from 5% to 69.4% depending on the precursor used.

Original languageEnglish (US)
Pages (from-to)807-815
Number of pages9
JournalHeterocycles
Volume95
Issue number2
DOIs
StatePublished - Jan 1 2017

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Microfluidics
Imaging techniques
Temperature
Processing
benzonitrile

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Pharmacology
  • Organic Chemistry

Cite this

Effect of leaving group substituents on the microfluidic synthesis of [18F]3-Fluoro-5-[(Pyridin- 3-YL)Ethynyl]benzonitrile ([18F]FPEB). / Moore, Thomas M.; Akula, Murthy; Collier, Lee; Tamagnan, Gilles; Papin, Caroline; Alagille, David; Kabalka, George.

In: Heterocycles, Vol. 95, No. 2, 01.01.2017, p. 807-815.

Research output: Contribution to journalArticle

Moore, Thomas M. ; Akula, Murthy ; Collier, Lee ; Tamagnan, Gilles ; Papin, Caroline ; Alagille, David ; Kabalka, George. / Effect of leaving group substituents on the microfluidic synthesis of [18F]3-Fluoro-5-[(Pyridin- 3-YL)Ethynyl]benzonitrile ([18F]FPEB). In: Heterocycles. 2017 ; Vol. 95, No. 2. pp. 807-815.
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