Issue 86, 2016, Issue in Progress
From the journal:

RSC Advances

Flow trifluoromethylation of carbonyl compounds by Ruppert–Prakash reagent and its application for pharmaceuticals, efavirenz and HSD-016†

Satoshi Okusu,a   Kazuki Hirano,a   Yoshimasa Yasuda,a   Etsuko Tokunagaa  and  Norio Shibata*a  

* Corresponding authors

a Department of Nanopharmaceutical Sciences & Department of Frontier Materials, Nagoya Institute of Technology, Gokiso, Showa-ku, Nagoya 466-8555, Japan
E-mail: nozshiba@nitech.ac.jp
Fax: +81-52-735-7543

Abstract

The Ruppert–Prakash reagent is the most powerful and well-documented reagent for trifluoromethylation. Despite its versatility, no general method exists for its use in a flow system. Here we report the first flow trifluoromethylation of carbonyl compounds and its utility for drug synthesis of efavirenz and HSD-016, including preliminary results of enantioselective variants.

Graphical abstract: Flow trifluoromethylation of carbonyl compounds by Ruppert–Prakash reagent and its application for pharmaceuticals, efavirenz and HSD-016

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Article information

DOI
https://doi.org/10.1039/C6RA19790F
Article type
Communication
Submitted
05 Aug 2016
Accepted
22 Aug 2016
First published
24 Aug 2016

RSC Adv., 2016,6, 82716-82720

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Flow trifluoromethylation of carbonyl compounds by Ruppert–Prakash reagent and its application for pharmaceuticals, efavirenz and HSD-016

S. Okusu, K. Hirano, Y. Yasuda, E. Tokunaga and N. Shibata, RSC Adv., 2016, 6, 82716 DOI: 10.1039/C6RA19790F

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