Issue 4, 2023

Micro-total process system machine (μ-TPSM) for rapid synthesis of antiretroviral darunavir

Abstract

Batch processes show great potential in antiretroviral darunavir (DRV) synthesis, but the longer process time, expensive catalyst, shortage of skilled manpower, laborious post-synthetic work-up, transport of one intermediate from one place to another, and need for maintaining expensive storage inventory are some major limitations. Herein, we report the first-ever individual continuous flow sequence involving 7 steps and an integrated micro-total process system machine (μ-TPSM) for the last 4 steps of API DRV synthesis. Employing this μ-TPSM, DRV could be synthesized within 41 min of total residence time with a 71% isolated yield, and an output of 0.8 g h−1. The use of RANEY®-Ni instead of palladium on carbon renders the process more affordable.

Graphical abstract: Micro-total process system machine (μ-TPSM) for rapid synthesis of antiretroviral darunavir

Supplementary files

Article information

Article type
Paper
Submitted
20 Oct 2022
Accepted
09 Jan 2023
First published
10 Jan 2023

React. Chem. Eng., 2023,8, 908-916

Micro-total process system machine (μ-TPSM) for rapid synthesis of antiretroviral darunavir

R. Chauhan, A. Rana, S. Ghosh, P. Srihari and A. K. Singh, React. Chem. Eng., 2023, 8, 908 DOI: 10.1039/D2RE00446A

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