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Synthesis 2024; 56(04): 603-610
DOI: 10.1055/s-0042-1751437
DOI: 10.1055/s-0042-1751437
special topic
Synthetic Development of Key Intermediates and Active Pharmaceutical Ingredients (APIs)
Synthesis of Ledipasvir through a Late-Stage Cyclopropanation and Fluorination Process
Financial assistance from Council of Scientific and Industrial Research is gratefully acknowledged [CSIR mission mode project (HCP-0011)].
Abstract
We have designed and developed an easily accessible advanced intermediate of ledipasvir that allowed late-stage cyclopropanation and difluorination, thereby providing a novel and more efficient process for the preparation of ledipasvir in the longest linear sequence of 8 steps with 20% overall yield.
Key words
ledipasvir - hepatitis C virus - late-stage fluorination - late-stage cyclopropanation - Boc-4-methylene-l-proline - harvoni - direct-acting antiviralsSupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0042-1751437.
- Supporting Information
Publication History
Received: 21 October 2022
Accepted after revision: 27 February 2023
Article published online:
13 April 2023
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