Lesinurad – There are More Ways than One of Synthesizing the Drug

Abstract

Over the last several years significant efforts have been devoted, particularly in China, to develop new syntheses of Lesinurad. Virtually all key bonds in this molecule can now be created in many different ways, often in a very high yield. Although almost all of the chemistry examples presented in this review come from patent applications and as such have not been subjected to rigorous peer review, they may serve as an inspiration to solve analogous synthetic problems.However, the readers are encouraged to pay particular attention to the very recent trends in the literature which use multicomponent reactions and flow chemistry to minimize the environmental impact and achieve high yields of API at the same time. CONTENTS:1. Introduction 2. Discussion of synthetic strategies 2.1. The original synthesis 2.2. Linking the cyclopropyl group with the naphthalene ring 2.3 Formation of the triazole ring 2.4 Linking the triazole ring with the naphthalene core 2.5 Bromination of the triazole ring 2.6 Introduction of the thioglycolic side chain 2.7 Application of one-pot, multicomponent and flow chemistry for the synthesis of Lesinurad Conclusions(-)-1 (+)-1 Lesinurad (1, RDEA594)