Synthesis of Ledipasvir through a Late-Stage Cyclopropanation and Fluorination Process

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 antivirals

Publication History

Received: 21 October 2022

Accepted after revision: 27 February 2023

Article published online:
13 April 2023

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