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Short Paper | Special issue | Vol 105, No. 1, 2022, pp.544-555
Published online, 8th March, 2022
DOI: 10.3987/COM-21-S(R)9
Improved Synthesis of Naldemedine Tosylate and Crystal Structures of Four Related Solid Forms

Josef Spreitz, Thomas Gelbrich, Sven Nerdinger,* Marijan Stefinovic, and Ulrich J. Griesser

*Sandoz GmbH, Biochemiestrasse 10, 6250 Kundl, Austria

Abstract

The production of drug substances requires a robust and scalable process capable of delivering the active pharmaceutical ingredient (API) in excellent chemical and polymorphic purity. With this goal in mind we have developed an improved procedure for the preparation of naldemedine tosylate, which crystallizes directly from the reaction mixture as pure polymorph form II. Solid state studies revealed a series of additional new physical forms whose crystal structure have been determined by single-crystal X-ray diffraction.