4.6 Article

A one-pot multicomponent approach to a new series of morphine derivatives and their biological evaluation

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 15, Issue 37, Pages 7796-7801

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c7ob01924f

Keywords

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Funding

  1. National Natural Science Foundation of China [81602959, 81473074, 81673291]
  2. Science Foundation of Zhejiang Sci-Tech University [16062192-Y]
  3. Arthritis & Chronic Pain Research Institute, USA

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A novel and facile domino reaction has been developed to synthesize a variety of new derivatives from hydromorphone, amines and paraformaldehyde in good yields in a catalyst-free fashion with high atom efficiency. The products show a mixed MOR/DOR biological characteristic which makes them valuable for further study as opioid analgesics.

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