@misc{oai:repo.qst.go.jp:00076536,
 author = {Yamaguchi, Hiroshi and Sumi, Takuya and Kang, Jiyoung and Yamashiro, Keiichi and Okada, Maki and Tateno, Masaru and Yamaguchi, Hiroshi and Okada, Maki},
 month = {May},
 note = {Background and purpose
We excelled off-target binding using computer chemistry techniques and worked on the development of PET imaging agents that bind to glutamate transporter (GLT). Although a plurality of asymmetric carbons generated within the compound skeleton could be excluded by structure optimization, there was a problem with deprotection of the aspartic acid skeleton in the skeleton. This study aims at establishing synthesis reactions that do not require protection / deprotection reaction by Click-Reaction, recalculation of In Silico binding assay, and synthesis of obtained structural compounds.

Method
In silico binding assay we derive the predominant and ERα non-binding structure in GLT binding and have studied labeling by [18F] on synthesis and synthesizer.  In the structure reported earlier, there was a problem in deprotection of the aspartic acid skeleton in the skeleton. We examined the establishment of synthetic reactions that do not require protection / deprotection reaction by Click-Reaction.

Results and discussion
We have established a design and synthesis route for compounds excluding asymmetric positions. However, as the yield in the deprotection reaction was low, a synthesis reaction that did not require protection / deprotection reaction by Click-Reaction was established. At present, the labeling reaction is preparing for sequencing at the time of synthesis, label synthesis, and animal experiments., The International Conference on Fluorine Chemistry 2019},
 title = {Structural design of glutamate transporter 18F-PET agent and synthesis using Click-Reaction},
 year = {2019}
}