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Letters in Organic Chemistry

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ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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Research Article

Synthesis of First Generation Dendron, GABA Caged Bis-1,2 -(4- acetylphenylethynyl)-4,5-dimethoxybenzene for Photorelease Study

Author(s): André Barrella, Nia H. Rene, Kisha J. Ali, Jeonghee Kang and Jong I. Lee*

Volume 16, Issue 9, 2019

Page: [718 - 722] Pages: 5

DOI: 10.2174/1570178616666190226152021

Price: $65

Abstract

First generation dendron bis-1,2-(4-acetylphenylethynyl)-4,5-dimethoxybenzene with a photo cleavable linkage to (t-butyloxycarbonyl-γ-aminobutyric acid (t-Boc-GABA) was synthesized for photo release study to apply for drug delivery. Both the divergent method from the core, 1,2- dimethoxybenzene and the convergent method from p-hydroxyacetophenone were not successful to generate the final dendron product. The dendron with caged GABA was successfully synthesized via the convergent method by attaching the model drug GABA on p-hydroxyacetophenone before the final Sonogashira coupling on 1,2-dimethoxybenzene according to the modified convergent method.

Keywords: Phototrigger, dendrimer, dendron, drug delivery, GABA, convergent method.

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