All Categories (1-6 of 6)

1. Improved Continuous Flow Processing: Benzimidazole Ring Formation via Catalytic Hydrogenation of an Aromatic Nitro Compound

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   Contributor(s):: Chen, Jian, Przyuski, Katrin, Roemmele, Renee, Bakale, Roger P.

   In the development of a new route to bendamustine hydrochloride, the API in Treanda, the key benzimidazole intermediate 5 was generated via catalytic heterogeneous hydrogenation of an aromatic nitro compound using a batch reactor. Because of safety concerns and a site limitation on hydrogenation...

2. The Synthesis of Bromomethyltrifluoroborates through Continuous Flow Chemistry

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   Contributor(s):: Broom, Toby, Hughes, Mark, Szczepankiewicz, Bruce G., Ace, Karl, Hagger, Ben, Lacking, Gary, Chima, Ranjit, Marchbank, Graeme, Alford, Gareth, Evans, Paul, Cunningham, Christopher, Roberts, John C., Perni, Robert B., Berry, Malcolm, Rutter, Andrew, Watson, Simon A

   A continuous flow process was developed for the synthesis of potassium bromomethyltrifluoroborate, a key precursor for Suzuki–Miyaura coupling reagents. The continuous flow process was used to produce potassium bromomethyltrifluoroborate on scales from grams to kilograms, and the successful...

3. Continuous Flow-Facilitated CB2 Agonist Synthesis, Part 2: Cyclization, Chlorination, and Amination

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   Contributor(s):: Prieschl, Michael, Sagmeister, Peter, Moessner, Christian, Sedelmeier, Joerg, Williams, Jason D., Kappe, C. Oliver

   A new route to the cannabinoid receptor type 2 agonist, RG7774, has been developed circumventing an alkylation with poor regioselectivity as the final step. In the new synthetic route, this side chain is incorporated from the beginning. In this article, the development of the final four...

4. Application of Continuous Flow for DIBAL-H Reduction and n-BuLi Mediated Coupling Reaction in the Synthesis of Eribulin Mesylate

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   Contributor(s):: Fukuyama, Takashi, Chiba, Hiroyuki, Kuroda, Hirofumi, Takigawa, Teiji, Kayano, Akio, Tagami, Katsuya

   Here we examined the use of continuous flow conditions for the final assembly of eribulin mesylate aimed to avoid cryogenic condition. The diisobutylaluminum hydride reduction of ester 2 to aldehyde 3 and n-butyllithium-mediated coupling of aldehyde 3 and sulfone fragment 4 to produce...

5. The Concept of Chemical Generators: On-Site On-Demand Production of Hazardous Reagents in Continuous Flow

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   Contributor(s):: Dallinger, D, Gutmann, B, Kappe, CO

   CONSPECTUS: In recent years, a steadily growing number of chemists, from both academia and industry, have dedicated their Research Article to the development of continuous flow processes performed in milli- or microreactors. The common availability of continuous flow equipment at virtually all...

6. Characterization and Modeling of the Operating Curves of Membrane Microseparators

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   Contributor(s):: Yang, L, Weeranoppanant, N, Jensen, KF

   The membrane microseparator is a milliliter-scale flow chemistry module that continuously separates a biphasic flow through a PTFE microporous membrane. It has found a wide range of applications in the continuous manufacturing of active pharmaceutical ingredients and fine chemicals, especially...