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Application Notes
The following application notes show the range of things that are possible with the Vapourtec system.
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This example illustrates the use of the Vapourtec R-Series system to react dissolved gases under pressure without the use of scale limiting pressure reactors (e.g. Parr ‘bombs’). Here the SnAr displacement of an aryl fluoride with dimethylamine is described. |
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 Application Note 22- Continuous Reduction of N-Boc Protected Amines to N-Me Amines |
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This example illustrates the use of the Vapourtec R-Series system to carry out reactions with moisture sensitive, highly reactive reagents under flow conditions. It demonstrates how the proper drying procedure allows the Vapourtec R2 pump to handle this highly water sensitive reagent. |
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| Application Note 21- Michael Addition with Nitromethane |
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This example illustrates the use of the Vapourtec R-Series flow chemistry platform to safely process an extremely energetic, reactive intermediate. |
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| Application Note 20 - Ethoxycarbonylation of Unprotected Iodoindole with CO Gas | ||||||
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| This application note again illustrates the use of the new Vapourtec tube-in-tube gas reactor. Here we describe the catalytic ethoxycarbonylation of unprotected Ioindole with CO gas, explaining the process of scaleup. | ||||||
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Request This Application Note>> Application Note 19 - Ethoxycarbonylation of Iodotoluene with CO Gas |
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| This application note illustrates the use of the new Vapourtec tube-in-tube gas reactor combined with the Vapourtec R-Series system to react reagent gases under pressure without the use of scale limiting pressure reactors (e.g. Parr ‘bombs’). Here we describe the catalytic ethoxycarbonylation of iodotoluene with CO gas. | ||||||
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This application note demonstrates the use of the newly launched Acid Resistant R Series flow system. (click here for more details). Highly corrosive fuming nitric acid is used in a nitration that is first optimised then scaled up to approx 50g/hr throughput. The whole study was completed with 2 days of installation of the Vapourtec instrument and took less than 8 hours of work, demonstrating the ease with which batch reactions can be converted to flow using the R Series. |
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| Application Note 16 - Bromination of Alkenes with NBS under continuous flow | ||||||
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| Bromination of unsaturated C-C bonds with NBS is a well known and widely used procedure, although when carried out in batch, slow and careful addition of the NBS is often required in order to prevent over-bromination & avoid thermal runaway. This study demonstrates how with flow chemistry these factors are no longer an issue. | ||||||
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| Application Note 15 - Bromination of Ketones | ||||||
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| Bromination with molecular bromine in batch mode usually requires slow and careful addition of the bromine reagent to control thermal kinetics, and often results in poor selectivity. This study demonstrates safe bromination in flow, giving rapid complete conversion and high selectivity. | ||||||
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| Application Note 14- Phase Transfer Catalysis | ||||||
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| Biphasic reactions, whereby the reaction takes place at the interface between two immiscible solvents, can be cleanly and reproducibly performed in a continuous flow reactor. This study demonstrates phase transfer catalyzed (PTC) alkylation of ß-Keto ester under segmented flow conditions. | ||||||
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| Application Note 1- Reaction Profiling using a 'Dual-Core™' Tubing Reactor | ||||||
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| An SNAr reaction using a continuous flow tubing reactor containing a dual core to illustrate reaction profiling. The smaller capacity reactor minimises sample wastage to obtain optimal reaction conditions that may be scaled-up in the larger reactor. | ||||||
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| Application Note 2- Optimisation of Step 1 in the Synthesis of Linezolid using a 'Dual-Core™' Tubing Reactor | ||||||
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| The smaller volume tubing reactor was used to determine optimal flow-through conditions suitable for the scale-up synthesis of the intermediate 3 required for the preparation of UpJohn's oxazolidinone antibiotic linezolid (Zyvox®). | ||||||
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| Application Note 3- Scale up SNAr using 12mL Tubing Reactor | ||||||
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| Example of the scaled-up preparation of SNAr using 12ml tubing reactor and 2 Knauer pumps. | ||||||
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| Application Note 4- Scale up SNAr using 4 Reactor Channels in Series | ||||||
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| Example of the scaled-up preparation of SNAr using the R-2PLUS Pumping Module and 4 x 10ml Tubing Reactors in series. | ||||||
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| Application Note 5- Heck C-C Coupling using Monolithic Nanoparticular Pd[0] PACT Reactor Cartridge | ||||||
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| Example of using the R-2PLUS Pumping Module and the R-2 Flow Reactor Heater with reactor columns to perform Polymer Assisted Continuous flow-Through (PACT) chemistry. | ||||||
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| Application Note 6- Transfer Hydrogenation using a Monolithic Nanoparticular Pd[0] PACT Reactor Cartridge | ||||||
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| Example of transfer Hydrogenation reactions using the R2+ Pumping Module and the R-4 Flow Reactor in combination with a reactor column without the need for Hydrogen gas. | ||||||
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| Application Note 7- Flow -Through Ester Hydrolysis under Superheated Conditions | ||||||
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| This Application Note illustrates how the R-2 pump/injector and R-4 flow reactor modules can bereadily used to perform flow-through chemistry under superheated conditions. | ||||||
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| Application Note 9- Amide Formation using 'Catch and Release' | ||||||
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| This Application Note illustrates how the R-2 pump/injector and R-4 flow reactor modules can be used to prepare amides uilising polymer-assisted continuous flow-through (PACT) chemistry. | ||||||
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| Application Note 10- Heterocycle Formation in Flow: 4,5-Disubstituted Oxazoles | ||||||
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| This Application Note illustrates how the R-2 pump/injector and R-4 flow reactor modules can beused to prepare oxazoles utilising a combination of a tubing reactor and polymer-assistedcontinuous flow-through (PACT) reactors | ||||||
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| Application Note 11- Array Synthesis using Loop Injection and a Tubing Reactor Combined with a Scavenger Column | ||||||
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| R2 pump/injector and R4 flow reactor module used with a flow reactor and a PACT scavenger column to perform sequential array synthesis employing simultaneous loop injection. | ||||||
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| Application Note 12- Weinreb Amidation | ||||||
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| Weinreb amidation, utilizing trimethylaluminium to activate amine for condensation with ester. Risky in batch due to pyrophoric reagent and potential thermal runaway with high energy intermediate, reaction is safely performed in a flow reactor with very short residence times, high yield and excellent conversion. | ||||||
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| Application Note 13- Suzuki Coupling | ||||||
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| A solid supported Pd catalyst column is used to perform a flow based Suzuki Coupling, synthesising *3-phenylpyridine***, with short residence time and high conversion. | ||||||
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