Abstract
AbstractA series of bicyclo analogues of several 2‐phenylmorpholines were synthesized and tested for anti‐tetrabenazine activity in mice. Most of the target compounds were prepared by reaction of 2‐bromopropio‐phenone (22) with the appropriate amino alcohol to form 2‐phenylmorpholinols. Reduction of the 2‐phenyl‐morpholinols with sodium borohydride gave amino diols, which were cyclized to morpholines with acid. Alternatively, oxazines 17 and 18 were synthesized by alkylation of phenyl‐(2‐pyrrolo)carbinol (32a) and phenyl‐(2‐piperidyl)carbinol (32b) with 2‐bromoethanol, followed by cyclization of the resulting amino diols with acid. Only the spirocyclic compounds 8 and 9 had i.p. anti‐tetrabenazine activity comparable to the non‐cyclic compounds 2a‐3b, but 8 and 9 were less active by the oral route of administration.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.