A one-pot multicomponent approach to a new series of morphine derivatives and their biological evaluation. Issue 37 (6th September 2017)

• Record Type: Journal Article
• Authors: 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
• Is Part Of: Organic & biomolecular chemistry. Volume 15:Issue 37(2017)
• Page Start: 7796
• Page End: 7801
• Publication Date: 2017-09-06
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c7ob01924f
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : Morphine derivatives displaying a mixed MOR/DOR biological characteristic were synthesized through a one-pot multicomponent approach. Abstract : 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.