Technical Name A METHOD OF SYNTHESIZING DENDRIMERIC AMPHIPHILE
Project Operator Kaohsiung Medical University
Project Host 高佳麟
Summary
A dendrimer amphiphile (DA) possesses hydrophobic and hydrophobic segments as well as branch structures. 
Herein, a solid-phase synthetic method was developed for their preparation. By using insoluble resin, the dendritic structure was prepared. With such insoluble resin, excess reagents were applied to complete reactions and suppressing side reactions. A safety-catch resin was used to introduce the aliphatic segment at the cleaving step which solves the controversial selection of solvent.
By controlling the amount of using the hydrophobic segment, desired products and remaining on-resin dendritic segments could be separated via simple filtration. Meanwhile, a cocktail solution was found as a crucial factor in this step. Moreover, microwave irradiation efficiently improve reaction yield and reduce reaction time.
This process generated desired products without chromatographic purification or repeated dialysis which are major obstruct in classical DA synthesis.
Scientific Breakthrough
A newly developed safety-catch resin was developed for the solid-phase synthesis of dendrimer amphiphiles. With this approach, their preparation could be divided into two parts-synthesis of hydrophobic and introduction of hydrophilic segments. Both segments could be individually synthesized and coupled together at the cleavage step. By controlling the amount of the hydrophobic segment, the desired product and remaining on-resin dendritic segment could separate through simple filtration. By using solid-phase synthetic methods, the dendritic structure was prepared on the resin. With such insoluble resin, excess reagents applied to increase the reactivity and suppressing the side reactions which improve yields and purity of dendritic products.
Industrial Applicability
Dendrimer amphiles (DA) have been used for the modification of nanoparticles and fabrication of semiconductors. Besides, the assembly bodies of DAs have been developed as nanoreactors for preparing regulated polymers and conducting efficient organic reactions. 
Regarding biomedical applications, regulated assembling ability was considered as an important property of good delivery vehicles. Assembly of DAs has been reported for delivering RNAi and imaging agents. They have reported being efficient antimicrobial agents and artificial vaccines.
With this reported skill, DAs, for the first time, reach the criteria of clinical applications. Meanwhile, this efficient method realized the systematic study of DA in biomedical applications which should identify more potential DAs in this regard.
Keyword self-assembly Amphiphilic molecules Dendrimer Solid-phase synthesis Delivery vehicles antimicrobial agents Vaccine Drugs Imaging agents Amphipihilic branched peptide
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