Synthesis of an Indoleamine-2,3-Dioxygenase-1 Inhibitor

Philip Kocienski
Synfacts, 2020, 16(07), 0758
https://doi.org/10.1055/s-0040-1707017

Abstract

Target molecule is an indoleamine-2,3-dioxygenase-1 inhibitor that is of interest for the treatment of cancer. Crystalline I was poorly soluble with low bioavailability but the highly bioavailable phosphonooxymethyl prodrug L and its crystalline tris-salt N were rapidly converted into I in vivo.

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