Metal-Free Synthesis of the Methanol Solvate of (S)-Omeprazole Potassium Salt Using (1R)-(−)-10-Camphorsulfonyloxaziridine: Oxidation Process Development and Optical Purity Enhancement Strategy

OPR&D March 2018


The results of our process development studies to synthesize the methanol solvate of (S)-omeprazole potassium salt (1) through the enantioselective oxidation of pyrmetazole (2) using (1R)-(−)-10-camphorsulfonyloxaziridine (3) are reported. Optical purity enhancement was achieved by means of a reslurry from methanol, the rationale and development details of which are also described.

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OPR&D - Minakem

Authors: Christine Delsarte, Romuald Santraine, Baptiste Fours*, and Laurent Petit* –

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Minakem Recherche, 145 Chemin des Lilas, 59310 Beuvry la Forêt, France
Source: Org. Process Res. Dev., 2018, 22 (3), pp 321–327

DOI: 10.1021/acs.oprd.7b00362
Publication Date (Web): March 2, 2018
Copyright © 2018 American Chemical Society

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