Synthesis of enantiopure 3-substituted morpholines |
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Authors: | Bornholdt Jan Felding Jakob Kristensen Jesper Langgaard |
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Affiliation: | Department of Medicinal Chemistry, University of Copenhagen, Universitetsparken 2, Copenhagen DK-2100, Denmark. |
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Abstract: | Enantiopure 3-substituted morpholines were assembled through ring-opening of a N-2-benzothiazolesulfonyl (Bts) activated aziridine with organocuprates followed by a ring annulation reaction with a vinylsulfonium salt under microwave conditions. Deprotection of the N-Bts group proceeds under very mild conditions with 2-mercaptoacetic acid and LiOH at rt. |
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