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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 36, 2006 - Issue 24
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Original Articles

One‐Pot Synthetic Procedure for2,2′‐Disubstituted Biaryls via the Suzuki Coupling Reaction of Aryl Triflates in a Biphasic Solvent System

Masanori Miura Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba‐shi, Ibaraki, JapanCorrespondence[email protected]
,
Takanori Koike Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba‐shi, Ibaraki, Japan
,
Tsukasa Ishihara Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba‐shi, Ibaraki, Japan
,
Fukushi Hirayama Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba‐shi, Ibaraki, Japan
,
Shuichi Sakamoto Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba‐shi, Ibaraki, Japan
,
Minoru Okada Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba‐shi, Ibaraki, Japan
,
Mitsuaki Ohta Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba‐shi, Ibaraki, Japan
&
Shin‐ichi Tsukamoto Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba‐shi, Ibaraki, Japan
 show all
Pages 3809-3820 | Received 23 Feb 2006, Published online: 01 Dec 2006
 
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Abstract

A one‐pot synthetic procedure for 2,2′‐disubstituted biaryls was developed via a Suzuki cross‐coupling reaction of aryl triflates in a biphasic solvent system. The effects of various bases and solvents were investigated. Results showed that the Na2CO3–toluene/H2O combination gave the highest yields.

Acknowledgment

The authors acknowledge Yuji Koga for his many helpful discussions during the preparation of this manuscript. We are also grateful to the staff of the Division of Analytical Science Laboratories of Astellas Pharma Inc. for elemental analysis and spectral measurements.

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