METHOD OF SYNTHESIZING N-CARBOXYANHYDRIDE USING FLOW REACTOR
PROBLEM TO BE SOLVED: To provide a synthesis method that allows high-yield continuous production of a compound of interest in synthesis and production of N-carboxyanhydride (NCA) and the like using a flow reactor. SOLUTION: In a synthesis method using a flow reactor 100, a basic solution adjusted in advance to a pH of 7-14 becomes acidic with a pH of 0-7, or an acidic solution adjusted in advance to a pH of 0-7 becomes basic with a pH of 7-14, within 60 seconds after the start of mixture of at least two ingredient solutions. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPOandINPIT
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Paragraph 0092-0096; 0111-0112
(2020/03/26)
Rapid and Mild Synthesis of Amino Acid N-Carboxy Anhydrides: Basic-to-Acidic Flash Switching in a Microflow Reactor
Polymerization of N-carboxy anhydrides (NCAs) is the primary process used to prepare polypeptides. The synthesis of various pure NCAs is key to the efficient synthesis of polypeptides. The only practical method that can be used to synthesize NCAs requires harsh acidic conditions that make acid-labile substrates unusable and results in an undesired ring opening of NCAs. Basic-to-acidic flash switching and subsequent flash dilution technology in a microflow reactor was used to demonstrate the synthesis of NCAs. It is both rapid (0.1 s) and mild (20 °C) and includes substrates containing acid-labile functional groups. The basic-to-acidic flash switching enabled both an acceleration of the desired NCA formation and avoided the undesired ring opening of NCAs. The flash dilution precluded the undesired decomposition of acid-labile functional groups. The developed process allowed the synthesis of various NCAs which cannot be readily synthesized using conventional batch methods.
Otake, Yuma,Nakamura, Hiroyuki,Fuse, Shinichiro
supporting information
p. 11389 - 11393
(2018/08/28)
Dendritic polypeptide-based nanocarriers for the delivery of therapeutic agents
Dendritic polypeptides useful for the delivery of therapeutic agents into cells are disclosed, together with their methods of preparation. These dendritic polypeptides serve as carriers of drugs, siRNA, aptamers and plasmid DNA in the treatment of various
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Page/Page column 17; 18
(2018/04/25)
A New Approach to the Preparation of N-Carboxy α-Amino Acid Anhydrides
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Mobashery, Shahriar,Johnston, Michael
p. 2200 - 2202
(2007/10/02)
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