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

Jiaan Shao; Richard A. Houghten; Colette T. Dooley; Margret Cazares; Jay P. McLaughlin; Shainnel O. Eans; Michelle L. Ganno; Michelle R. Hoot; Marc A. Giulianotti; Yongping Yu

doi:10.1039/C7OB01924F

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

Jiaan Shao,*^a Richard A. Houghten,^b Colette T. Dooley,

^b Margret Cazares,^b Jay P. McLaughlin,^b Shainnel O. Eans,^b Michelle L. Ganno,^b Michelle R. Hoot,^b Marc A. Giulianotti*^b and Yongping Yu

*^bc

Author affiliations

* Corresponding authors

^a Department of Chemistry, Zhejiang Sci-Tech University, Hangzhou, Zhejiang 310018, P. R. China
E-mail: shaojia_an@126.com

^b Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, Florida 34987, USA
E-mail: Marcello@tpims.org

^c College of Pharmaceutical Science, Zhejiang University, Hangzhou, Zhejiang 310058, P. R. China
E-mail: yyu@zju.edu.cn

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.

Organic & Biomolecular Chemistry

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

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

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