Stereoretentive Etherification of an α-Aryl-β-amino Alcohol Using a Selective Aziridinium Ring Opening for the Synthesis of AZD7594
A selective aziridinium ring-opening was used to etherify an α-aryl-β-amino alcohol with stereochemical retention. This transformation was achieved in a biphasic system to address phenoxide solubility and the formation of a sulfonate ester impurity.
Unit Operation: Mixing, Process
Objective: Modeling
Company: AstraZeneca, Dept. of Chemistry and Applied Biosciences, Zurich
Source: J. Org. Chem., Article ASAP
Authors: Ian W. Ashworth (AstraZeneca), Lai C. Chan (AstraZeneca), Maria Rita Galan Espinosa (AstraZeneca), Martin F. Jones (AstraZeneca), Angus E. McMillan (Dept. of Chemistry and Applied Biosciences, Zurich), Alexander K. Mullen (AstraZeneca), Michael J. Pilling (AstraZeneca), Steven A. Raw (AstraZeneca), Alan Steven (AstraZeneca)
Publish Date: 19-Jun-2018
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