Concise synthesis of 3,7-dioxa-9-aza-bicyclo[3,3,1]-nonane |
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Authors: | Park Cheol-Min |
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Affiliation: | Cancer Research, Global Pharmaceutical R&D, Abbott Laboratories, 100 Abbott Park Rd., Abbott Park, Illinois 60064, USA. cheol-min.park@abbott.com |
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Abstract: | [reaction: see text] The basicity of an amine has a great impact on physicochemical properties and pharmacokinetics. To attenuate the basicity of morpholine, a bicyclic amine was designed and synthesized with the introduction of an additional beta-oxygen. A transannular cyclization and reduction of a bridgehead alpha-chloro amine functionality produces the topographically unusual amine (pKa = 6.7) in good yield. |
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