All Categories (1-3 of 3)

1. Synthesis of treprostinil: key Claisen rearrangement and catalytic Pauson–Khand reactions in continuous flow

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   10 May 2024 | Contributor(s):: García-Lacuna, Jorge, Domínguez, Gema, Blanco-Urgoiti, Jaime, Pérez-Castells, Javier

   A new synthesis of treprostinil is described using a plug flow reactor in two of the key steps. First, a Claisen rearrangement reaction is described in scaled flow at multigram amounts. Yields and selectivity of this step are sharply improved compared to those from previous syntheses. Second, the...

2. Pilot-Scale Continuous Production of LY2886721: Amide Formation and Reactive Crystallization

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   10 May 2024 | Contributor(s):: Polster, Christopher S., Cole, Kevin P., Burcham, Christopher L., Campbell, Bradley M., Frederick, Andrea L., Hansen, Marvin M., Harding, Molly, Heller, Michael R., Miller, Michael T., Phillips, Joseph L., Pollock, Patrick M., Zaborenko, Nikolay

   The design, development, and implementation of a pilot-scale continuous Schotten–Baumann amide bond formation and reactive crystallization to afford LY2886721 is described. The material met all API quality attributes and was comparable to material produced by a defined batch process. The...

3. Scaling continuous API synthesis from milligram to kilogram: extending the enabling benefits of micro to the plant

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   09 Jun 2023 | Contributor(s):: Berton, M, de, Souza, JMAbdiaj, I, McQuade, DT, Snead, DR

   The signature benefits of continuous flow are largely a result of a reactor's micro-sized features. However, as the technology gains industrial traction in the synthesis of active pharmaceutical ingredients (API), the reactors must be scaled to larger size to meet production demands. Often, the...