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

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

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...

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Veröffentlicht in:Organic & biomolecular chemistry 2017-09, Vol.15 (37), p.7796-7801
Hauptverfasser: Shao, Jiaan, Houghten, Richard A, Dooley, Colette T, Cazares, Margret, McLaughlin, Jay P, Eans, Shainnel O, Ganno, Michelle L, Hoot, Michelle R, Giulianotti, Marc A, Yu, Yongping
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Sprache:eng
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Zusammenfassung: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.
ISSN:1477-0520
1477-0539
DOI:10.1039/c7ob01924f