Concepedia

Rapid Development of a Commercial Process for Linrodostat, an Indoleamine 2,3-Dioxygenase (IDO) Inhibitor

Kenneth J. Fraunhoffer, Albert J. DelMonte, Gregory L. Beutner, Michael Bultman, Kathryn M. Camacho, Benjamin Cohen, Darryl D. Dixon, Yu Fan, Dayne Fanfair, Adam Freitag,

Organic Process Research & Development · 2019 · 38 citations · 21 references

DOI

Concepts

Abstract

The process development and the kilogram-scale synthesis of linrodostat (BMS-986205, 1) are described. The synthesis features several highly efficient telescoped processes and the use of Evans auxiliary to install a methyl-bearing stereocenter. The target was prepared in 12 steps with 7 isolations in an overall yield of 31%.

References

21

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Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form

Micah T. Nelp, Patrick A. Kates, John T. Hunt et al. · Proceedings of the National Academy of Sciences · 2018 · 208 citations · Full text

, , +14