Issue 32, 2017, Issue in Progress
From the journal:

RSC Advances

Synthesis and biological evaluation of fentanyl acrylic derivatives†

Shaohua Li,ab   Devora Cohen-Karni,ab   Marina Kovaliov,ab   Nestor Tomycz,b   Boyle Cheng,b   Donald Whitingb  and  Saadyah Averick ORCID logo *ab  

* Corresponding authors

a Neuroscience Disruptive Research Lab, Allegheny Health Network Research Institute, Allegheny General Hospital, Pittsburgh, Pennsylvania 15212, USA
E-mail: Saadyah.Averick@ahn.org
Tel: +1-412-359-4943

b Neuroscience Institute, Allegheny Health Network, Allegheny General Hospital, Pittsburgh, Pennsylvania 15212, USA

Abstract

The synthesis of novel fentanyl acrylate derivatives via bromo-fentanyl using Heck coupling is described. The synthesis is concise and represents an efficient and useful method for functionalizing fentanyl for medicinal chemistry investigations. The agonistic and analgesic activities are evaluated by Mu opioid receptor activation and hot plate assays in mice.

Graphical abstract: Synthesis and biological evaluation of fentanyl acrylic derivatives

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Article information

DOI
https://doi.org/10.1039/C7RA01346A
Article type
Paper
Submitted
01 Feb 2017
Accepted
24 Mar 2017
First published
05 Apr 2017
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2017,7, 20015-20019

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Synthesis and biological evaluation of fentanyl acrylic derivatives

S. Li, D. Cohen-Karni, M. Kovaliov, N. Tomycz, B. Cheng, D. Whiting and S. Averick, RSC Adv., 2017, 7, 20015 DOI: 10.1039/C7RA01346A

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