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Publication No: IN202311007990 [India] Application No: 202311007990
Title: An integrated continuous flow synthesis of anti-retroviral drug Darunavir
Publication Date: 09-08-2024 File Date: 07-02-2023
Inventor(s): Ajay Kumar Singh; Subhash Ghosh; Srihari Pabbaraja; Ruchi Chauhan; Abhilash Rana
IPC Classification: B01J 19/00, A61K 9/16, A61P 31/18, A61K 9/20, B01D 53/62
Abstract:
Batch process shows great potential in antiretroviral drug Darunavir (DRV) synthesis, but the longer process time, expensive catalyst, huge manpower, highly laborious  post-synthetic work-up, transport of one intermediate from one place to another, and need of huge storage capacity are some major limitations. Herein, we report first- ever individual continuous flow process involving 7 steps and an integrated micro-total process system for the last 4 steps of API DRV synthesis. Employing this  process, DRV could be synthesize within 41 min. of total residence time with 71% yield. The use of Raney-Ni instead of palladium on carbon renders metal the process  more affordable. Present invention describes a new synthetic approach toward automated, scalable synthesis that combines techniques in automated separation, solvent  exchange and one common solvent to continue for multi-step reaction.
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Industrial Applications Chemistry, Chemical Processes Polymers [Chemistry, Chemical Processes] Synhtesis Procesess [Drugs and Pharmaceuticals]