Radiation induced oxidation of [¹⁸F]fluorothia fatty acids under cGMP manufacturing conditions.

ABSTRACT:

Objective

The objectives of the present work were to optimize and validate the synthesis and stability of 14(R,S)-[¹⁸F]fluoro-6-thia-heptadecanoic acid ([¹⁸F]FTHA) and 16-[¹⁸F]fluoro-4-thia-palmitic acid ([¹⁸F]FTP) under cGMP conditions for clinical applications.

Methods

Benzyl-14-(R,S)-tosyloxy-6-thiaheptadecanoate and methyl 16-bromo-4-thia-palmitate were used as precursors for the synthesis of [¹⁸F]FTHA and [¹⁸F]FTP, respectively. For comparison, a fatty acid analog lacking a thia-substitution, 16-[¹⁸F]fluoro-palmitic acid ([¹⁸F]FP), was synthesized from the precursor methyl 16-bromo-palmitate. A standard nucleophilic reaction using cryptand (Kryptofix/K222, 8.1 mg), potassium carbonat

SUBMITTER: Pandey MK 

PROVIDER: S-EPMC7056516 | biostudies-literature | 2020 Jan - Feb

REPOSITORIES: biostudies-literature