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| Open AccessMirror-image ligand discovery enabled by single-shot fast-flow synthesis of D-proteins
Mirror-image phage display has the potential for high-throughput generation of biologically stable macrocyclic D-peptide binders but is hindered by the optimization required for D-protein chemical synthesis. Here, the authors report a general mirror-image phage display pipeline based on automated flow peptide synthesis and use it to prepare and characterize 12 L/D-protein pairs.
- Alex J. Callahan
- , Satish Gandhesiri
- & Bradley L. Pentelute
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Article
| Open AccessDynamic metastable polymersomes enable continuous flow manufacturing
Polymersomes, as analogues of liposomes, have interesting physical and chemical properties, but have not yet been translated into clinical or industrial applications. Here, the authors report the development of a continuous flow process for the production of polymersomes at scale.
- Chin Ken Wong
- , Rebecca Y. Lai
- & Martina H. Stenzel
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Article
| Open AccessEx-situ generation and synthetic utilization of bare trifluoromethyl anion in flow via rapid biphasic mixing
The trifluoromethyl anion rapidly decomposes into difluorocarbene (:CF2) and fluorine ion, limiting its applicability in synthesis. Here, the authors report a strategy to generate and use the short-lived CF3- intermediate from stable CF3H gas via fast biphasic mixing in precisely customized flow dissolvers.
- Hyune-Jea Lee
- , Jeong-Un Joo
- & Heejin Kim
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Article
| Open AccessInterfacial solute flux promotes emulsification at the water|oil interface
Emulsions are critical across a broad spectrum of industries. Here authors demonstrate a mechanism of spontaneous droplet formation, where the interfacial solute flux promotes droplet formation at the liquid-liquid interface when a phase transfer agent is present.
- Guillermo S. Colón-Quintana
- , Thomas B. Clarke
- & Jeffrey E. Dick
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Article
| Open AccessSolution-processable microporous polymer platform for heterogenization of diverse photoredox catalysts
Heterogeneous photocatalysts are easily separable and recyclable, but homogeneous ones are precisely tunable. Here, the authors merge the benefits of these two catalyst types by incorporating diverse dyes into solution-processable, porous polymers.
- Richard Y. Liu
- , Sheng Guo
- & Timothy M. Swager
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Article
| Open AccessElectrochemical C–H phosphorylation of arenes in continuous flow suitable for late-stage functionalization
Synthesis of aryl phosphorus compounds with electron-withdrawing substituents on the arene is difficult to do simply. Here the authors show a method to form aryl carbon-phosphorus bonds through electrochemistry, without requiring any catalyst or external oxidant.
- Hao Long
- , Chong Huang
- & Hai-Chao Xu
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Article
| Open AccessFully automated fast-flow synthesis of antisense phosphorodiamidate morpholino oligomers
PMOs (phosphorodiamidate morpholino oligomers) have huge potential for antisense therapy but complex and slow synthesis limits application. Here, the authors report the development of automated flow synthesis methods which reduce nucleobase coupling times from hours to minutes removing human errors and allow for high-throughput production.
- Chengxi Li
- , Alex J. Callahan
- & Bradley L. Pentelute
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| Open AccessA droplet microfluidic platform for high-throughput photochemical reaction discovery
Translating discovery scale vial-based batch reactions to continuous flow scale-up conditions is limited by significant time and resource constraints. Here, the authors report a photochemical droplet microfluidic platform, which enables high throughput reaction discovery in flow to generate pharmaceutically relevant compound libraries.
- Alexandra C. Sun
- , Daniel J. Steyer
- & Corey R. J. Stephenson
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Article
| Open AccessDirect electrochemical oxidation of alcohols with hydrogen evolution in continuous-flow reactor
Alcohol oxidation to carbonyl compounds is a very useful functional group transformation in organic synthesis. Here, the authors perform the direct electrochemical oxidation of various alcohols to the corresponding ketones in a continuous-flow reactor without external oxidants, base or mediators.
- Dan Wang
- , Pan Wang
- & Aiwen Lei
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Article
| Open AccessAccelerated microfluidic native chemical ligation at difficult amino acids toward cyclic peptides
Flow-based peptide synthesis is a well-established method, yet difficult to combine with native chemical ligation (NCL), the go-to method for peptide cyclization. Here, the authors developed a microfluidic procedure for peptide cyclization within minutes, using NCL and an SEA alkylthioester peptide.
- Nathalie Ollivier
- , Thomas Toupy
- & Oleg Melnyk
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Article
| Open AccessTotal synthesis of feglymycin based on a linear/convergent hybrid approach using micro-flow amide bond formation
Feglymycin is a biologically active peptide but a challenging synthetic target due to the highly racemizable nature of the 3,5-dihydroxyphenylglycine groups. Here the authors report the synthesis of feglymycin using a microflow system, allowing amide bond formation without severe racemization.
- Shinichiro Fuse
- , Yuto Mifune
- & Hiroshi Tanaka
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Article
| Open AccessControlled multistep synthesis in a three-phase droplet reactor
Droplet chemistry is less susceptible to channel-fouling than single-phase flow chemistry, but is largely limited to simple reactions where all reagents are preloaded into droplets. Here, the authors report a method for multistep chemistry in droplets, using two immiscible liquids and a gas to achieve controlled, sequential reagent addition.
- Adrian M. Nightingale
- , Thomas W. Phillips
- & John C. de Mello