High-Yielding Automated Convergent Synthesis of No-Carrier-Added [C-]-Labeled Amino Acids Using the Strecker Reaction

Overview

Journal Synlett

Specialty Chemistry

Date 2018 Feb 13

PMID 29430080

Citations 7

Authors

Junhao Xing

Allen F Brooks

Dylan Fink

Huibin Zhang

Morand R Piert

Peter J H Scott

Xia Shao

Affiliations

Soon will be listed here.

Abstract

A new variant of the Strecker synthesis using no-carrier-added [C]cyanide for the synthesis of radiolabeled amino acids is described. The protocol is fully automated using a radiochemistry synthesis module and applied to the production of a number of new PET radiotracers. [C-]sarcosine, [C-]methionine, [C-]--phenylglycine, and [C-]glycine are all synthesized in moderate to good radiochemical yields. The synthesis of [C-]sarcosine has been validated for production of doses for clinical use, and preliminary evaluation of the new radiotracer in PC3 tumor-bearing mice is also reported.

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