A convenient and reproducible method for the synthesis of astatinated 4-[ <sup>211</sup> At]astato- <scp>l</scp> -phenylalanine <i>via</i> electrophilic desilylation

Watanabe, Shigeki; Anwar-ul Azim, Mohammad; Nishinaka, I.; Sasaki, Ichiro; Ohshima, Yasuhiro; Yamada, Keiichi; S. Ishioka, Noriko

doi:10.1039/c8ob02394h

Public

A convenient and reproducible method for the synthesis of astatinated 4-[ 211 At]astato- l -phenylalanine via electrophilic desilylation

Published in Organic & Biomolecular Chemistry • Dec 4, 2018

Authors:

Shigeki Watanabe

Mohammad Anwar-ul Azim

I. Nishinaka

Abstract

The 211At-labeled compound, 4-[211At]astato-l-phenylalanine, is one of the most promising amino acid derivatives for use in targeted alpha therapy (TAT) for various cancers. Electrophilic demetallation of a stannyl precursor is the most widely used approach for labeling biomolecules with 211At. Howe...

Subject

Electrophile

Phenylalanine

Chemistry

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